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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 21. Отображено 21.
16-05-2023 дата публикации

Synthesis method of semeglutide

Номер: CN116120427A
Автор: WEI XI, DENG DEXIONG, LI YUANQIANG, LIN KEWEI, ZHANG QIDONG, YU CHUAN, YANG HANBING, XU FENG
Принадлежит:

The invention provides a synthetic method of semeglutide. Comprising the following steps: sequentially coupling amino acids or peptide fragments from a C terminal to an N terminal according to an amino acid sequence of the semeglutide through a solid-phase synthesis method to obtain semeglutide full-protection resin, and cracking and purifying to obtain the semeglutide, the peptide fragment comprises a dipeptide S20-S21 formed by 20-21st amino acids, the S20-S21 is R1-Lys (Fmoc)-Glu (OtBu)-OH, R1 is Dde or ivDde, Fmoc is a side chain protecting group, and R1 is a main chain protecting group. The total yield of the crude product of the semeglutide reaches 57.07%, the HPLC (high performance liquid chromatography) purity reaches 77.71%, impurities are reduced, the production, synthesis and purification processes are simple, the selected materials are cheap and easy to obtain, the comprehensive production cost is low, and industrial production is facilitated.

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Номер записи: 1
21-08-2014 дата публикации

CRIZOTINIB PREPARATION METHOD

Номер: WO2014124594A1
Автор: LI, Yuanqiang, QIAN, Jianqiang, CHE, Daqing
Принадлежит:

The present invention relates to the field of pharmaceutical synthesis, in particular to a crizotinib preparation method. The method is a preparation method of a compound having a structure of formula (a): conducting Suzuki coupling reaction between a compound having a structure of formula (b) and a compound having a structure of formula (e) to obtain the compound having the structure of formula (a); further conducting a deprotection reaction on the compound having the structure of formula (a) to obtain (±) crizotinib.

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Номер записи: 2
04-07-2023 дата публикации

Preparation method of chiral iron complex

Номер: CN116375771A
Автор: LUO LIJUN, LI YUANQIANG, XU WEIZE, CHEN QIAN, CHEN XIAOMIN
Принадлежит:

The invention discloses a preparation method of a chiral iron complex. The preparation method comprises the following steps: introducing a solution 1 containing an iron precursor and a solution 2 containing alpha-diazophenylacetic acid methyl ester into a continuous flow preparation system for preparation, wherein the continuous flow preparation system is used for monitoring and adjusting the ratio of an iron-containing precursor to alpha-diazophenylacetic acid methyl ester to be optimal in real time; compared with the prior art, the method has the advantages that the solution 1 containing the iron precursor and the solution 2 containing the alpha-diazophenylacetic acid methyl ester are introduced into the continuous flow preparation system for industrial reaction, and the ratio of the iron precursor to the alpha-diazophenylacetic acid methyl ester is monitored and adjusted in real time; compared with the prior art, the method has the advantages that accumulation of methyl alpha-diazophenylacetate ...

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Номер записи: 3
24-03-2016 дата публикации

ASYMMETRICAL HYDROGENATION REACTION OF KETONIC ACID COMPOUND

Номер: WO2016041351A1
Автор: YAN, Pucha, LI, Yuanqiang, CHE, Daqing, ZHANG, Xiangdong, CHEN, Kang, YAN, Yongliang
Принадлежит:

The present invention relates to the technical field of organic chemistry, specifically an asymmetrical hydrogenation reaction of an α-ketonic acid compound, the scheme being as shown by formula (I), wherein R1 is a phenyl, a substituted phenyl, a naphthyl, a substituted naphthyl, a C1-C6 alkyl or an aralkyl; the substituent is a C1-C6 alkyl, a C1-C6 alkoxy, a halogen; and the number of the substituents is 1-3. M is a chiral spiro-pyridylamidophosphine ligand iridium complex having the structure (II), wherein R is hydrogen, 3-methyl, 4-tBu or 6-methyl.

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Номер записи: 4
03-07-2014 дата публикации

METHOD FOR PREPARING EZETIMIBE CHIRAL INTERMEDIATE

Номер: WO2014101690A1
Автор: YAN, Pucha, CHE, Daqing, LI, Yuanqiang, ZHU, Guoliang, ZHANG, Xiangdong, QU, Xiaoguang
Принадлежит:

The present invention relates to the field of pharmaceutical synthesis, and specifically, to a method for preparing an Ezetimibe chiral intermediate. The method is as follows: a method for preparing a compound with a formula (b) structure comprises the following steps: obtaining the compound with the formula (b) structure by using a compound with a formula (a) structure under the effects of a chiral catalyst, alkali and hydrogen, R is NR１R2, OR3 or OH, R１ and R2 are separate alkyl groups, and R3 is an C1-C6 alkyl group or a benzyl group. The chiral catalyst is a compound with a formula (M) structure: DTB is shown as a formula DTB. The yield of the compound with the formula (b) prepared by using the method can exceed 95%, and the optical purity can reach 100% at the maximum.

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Номер записи: 5
02-05-2023 дата публикации

Chiral spirobiindene ligand as well as preparation method and application thereof

Номер: CN116041207A
Автор: YAN PUCHA, ZHOU BO, CHENG HOU'AN, HUA YUNYU, SONG LINGJIE, ZHANG YU, CHEN BIN, LI YUANQIANG
Принадлежит:

The invention provides a chiral spirobiindane ligand as well as a preparation method and application thereof. The chiral spirobiindene ligand is a compound shown in a formula A or acceptable salt thereof, in the formula A, R1 is selected from one of hydrogen, alkyl, alkoxy, aryl and heteroaryl, and R2 is selected from one of alkyl, alkoxy, aryl and heteroaryl. The chiral spirobiindene ligand disclosed by the invention has high selectivity, high yield and wide substrate applicability.

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Номер записи: 6
18-04-2023 дата публикации

Method for preparing sacubitril compound through asymmetric catalytic hydrogenation

Номер: CN115974634A
Автор: YAN PUCHA, ZHOU BO, HUA YUNYU, CHENG HOU'AN, HU YONGJIANG, LI YUANQIANG
Принадлежит:

The invention discloses a method for preparing a sacubitril compound through asymmetric catalytic hydrogenation. The method is an industrial production route. The invention relates to a route for synthesizing a sacubitril compound through an asymmetric catalytic hydrogenation reaction.

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Номер записи: 7
04-07-2013 дата публикации

SILODOSIN INTERMEDIATE AND PREPARATION METHOD THEREFOR

Номер: WO2013097456A1
Автор: ZHANG, Bin, HU, Xiaowei, YAN, Pucha, ZHANG, Xianyi, GAO, Hongjun, LI, Yuanqiang, CHE, Daqing
Принадлежит:

Disclosed are a silodosin intermediate and a preparation method therefor. The silodosin intermediate has the structure shown by the formula (A). X is hydrogen or bromine and R1 is hydrogen. The formyl group may be a group having the structure shown by the formula I. R7 is an acid protecting group, and R2 is 3-hydroxypropyl or a group having the structure shown by the formula II. W is an alcohol protecting group. A compound of the formula (A) according to the present invention may further be used for preparing a compound having the structure shown by the formula (D). By means of the intermediate and the preparation method therefor provided by the present invention, high-purity optically pure silodosin can be obtained, and the optical purity is above 99%.

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Номер записи: 8
11-07-2023 дата публикации

Asymmetric hydrogenation reaction of alkenyl keto ester compound

Номер: CN116410142A
Автор: YAN PUCHA, XIE JIANHUA, ZHOU BO, BIN HUAIYU, ZHU JIAWEN, GAO YANG, HUA YUNYU, LI YUANQIANG
Принадлежит:

The invention relates to the technical field of organic chemistry, in particular to an asymmetric hydrogenation reaction of an alkenyl keto ester compound, and the technical scheme is as follows: a chiral catalyst is a chiral spiro pyridine amine phosphine iridium complex. The technical scheme provided by the invention has the technical advantages of small catalyst dosage, high catalytic product yield, high chiral purity and the like, so that the method is suitable for industrial production.

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Номер записи: 9
23-06-2023 дата публикации

Method for synthesizing polypeptide drugs

Номер: CN116284238A
Автор: XU FENG, WEI XI, LI YUANQIANG, DENG DEXIONG, DONG SHI, CAI JIN, YAO WEIWEI, YU CHUAN
Принадлежит:

The invention provides a method for synthesizing a polypeptide drug. Comprising the following steps: (1) amino acid coupling reaction: in a reaction medium, carrying out coupling reaction on a non-classical solid-phase synthesis carrier and Fmoc-amino acid under the action of a condensation reagent, concentrating, precipitating and filtering to obtain an Fmoc-peptide carrier; (2) Fmoc protecting group removal reaction: adding the Fmoc-peptide carrier into the deprotection liquid for deprotection reaction to obtain an extended peptide carrier; (3) repeating the steps (1) and (2) until all amino acids in the polypeptide drug are connected to obtain a polypeptide drug carrier; (4) adding the cutting fluid into the polypeptide drug carrier, settling and centrifuging to obtain the polypeptide drug; wherein the structure of the non-classical solid-phase synthesis carrier is shown in the following formula, and R is n-octadecyl. Large-scale production of polypeptide products can be realized, the ...

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Номер записи: 10
05-05-2023 дата публикации

Spirobiindane ligand as well as preparation method and application thereof

Номер: CN116063232A
Автор: YAN PUCHA, ZHOU BO, HUA YUNYU, CHENG HOU'AN, SONG LINGJIE, GAO YANG, CHEN BIN, LI YUANQIANG
Принадлежит:

The invention provides a spirobiindane ligand as well as a preparation method and application thereof. The ligand is a compound with a structure as shown in a formula E or an acceptable salt of the compound, R is selected from any one of hydrogen, alkyl, alkoxy, aryl and heteroaryl, and X is selected from C or O. The chiral spiro ligand synthesized for the first time is applied to asymmetric catalytic reaction, the yield is high, and the chemical selectivity is good; the method is wide in applicable substrate range, simple and convenient to operate and mild in reaction condition.

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Номер записи: 11
04-04-2023 дата публикации

Method for constructing C-P bond through nickel-catalyzed Hirao reaction

Номер: CN115894560A
Автор: HUANG LIN, HOU MEIFENG, ZHANG HANYUE, SANG QIHANG, LI YUANQIANG
Принадлежит:

The invention provides a method for constructing a C-P bond through a nickel-catalyzed Hirao reaction, which comprises the following steps: in the presence of a nickel catalyst, an additive and alkali, a substituted aryl compound 1 and diphenylphosphine oxide 2 are subjected to a coupling reaction in an organic solvent to generate an aryl phosphine oxide compound 3, and the reaction formula is as follows: X is any one of F, Cl, Br, I, OTf, B (OH) 2 and OCF3; and Ar is aryl. The method disclosed by the invention has the effects that the substrate has universality, the operation is simple, the condition is mild, a noble metal catalyst and a phosphine ligand are not needed, the cost is low, and the yield is high.

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Номер записи: 12
11-08-2023 дата публикации

Non-classical solid-phase synthesis carrier as well as preparation method and application thereof

Номер: CN116573992A
Автор: XU FENG, WEI XI, LI YUANQIANG, DENG DEXIONG, HU MEILING, DONG SHI, YAO WEIWEI, YANG HANBING
Принадлежит:

The invention discloses a non-classical solid-phase synthesis carrier as well as a preparation method and application thereof, the prepared non-classical solid-phase synthesis carrier not only realizes homogeneous coupling of a carrier or a peptide carrier and amino acid, but also can complete splitting decomposition in a splitting decomposition solution, and retains a side chain protecting group of the amino acid in a peptide chain at the same time; the synthesis of a polypeptide product and the full-protection cracking of an amino acid side chain are realized; under the same production scale, the volume of the reactor can be reduced by 30%-50%, the dosage of the raw material amino acid and the condensing agent is reduced by 50%-60%, the dosage of the organic solvent for reaction and washing is reduced by 60%-80%, and finally, the production cost is reduced by 50%-70%. The carrier prepared by the invention can realize synthesis of polypeptide products and full-protection cracking of amino ...

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Номер записи: 13
02-05-2023 дата публикации

Method for synthesizing diphenyl-2-pyridylmethane derivative

Номер: CN116041253A
Автор: YAN PUCHA, ZHOU BO, HAN XIAOQING, HUA YUNYU, ZHENG CONG, HU YONGJIANG, HU XIAOWEI, LI YUANQIANG
Принадлежит:

The invention provides a method for synthesizing a diphenyl-2-pyridyl methane derivative. A compound D, butylboronic acid, a catalyst, a ligand, an additive, an oxidizing agent and an organic solvent 1 are mixed and stirred for a reaction, the diphenyl-2-pyridylmethane derivative E is obtained through separation and purification, the chemical reaction formula of the diphenyl-2-pyridylmethane derivative E is shown in the specification, and R1 and R2 are respectively and independently selected from one of hydrogen, alkyl, alkoxy, aryl and heteroaryl. The method has the advantages of high selectivity, high yield, high reaction catalysis efficiency, low catalyst dosage, simple post-treatment and no generation of by-products in the system.

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Номер записи: 14
02-05-2023 дата публикации

Asymmetric C-H bond arylation reaction method of amide compound

Номер: CN116041216A
Автор: YAN PUCHA, ZHOU BO, HUA YUNYU, ZHENG CONG, HAN XIAOQING, CHENG HOU'AN, HU XIAOWEI, LI YUANQIANG
Принадлежит:

The invention provides a method for an asymmetric C-H bond arylation reaction of an amide compound. Comprising the steps that a compound shown in the formula 2, aryl fluoborate, a catalyst, a ligand, an additive, an oxidizing agent, alkali, water and a solvent are mixed and stirred under the nitrogen condition, a cross-coupling reaction is conducted, a target compound 1 is generated, the reaction equation is shown in the specification, R1 is one of alkyl, alkoxy, phenyl and substituted phenyl, and Ar is aryl or substituted aryl; and ArF is a fluorine-substituted aryl group. The chiral catalyst provided by the invention provides a new reaction way for asymmetric C-H activation of acyclic amide, has high selectivity and high yield, is mild in reaction condition, simple in method, green and environment-friendly, and is suitable for large-scale industrial production.

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Номер записи: 15
02-05-2023 дата публикации

Method for asymmetrically synthesizing cyclobutane derivative

Номер: CN116041204A
Автор: YAN PUCHA, ZHOU BO, ZHENG CONG, HUA YUNYU, HU YONGJIANG, LIN ZUPENG, LI YUANQIANG
Принадлежит:

The invention provides a method for asymmetrically synthesizing a cyclobutane derivative. A compound 2 and PhBpin are used as substrates and are mixed with a catalyst, a ligand, an additive, an oxidizing agent, alkali, water and a solvent for reaction to generate a target compound 1, and the reaction formula is as follows: R1 is selected from one of alkyl, alkoxy, aryl and heteroaryl. The chiral alpha-amino spiro ligand and the Pd (II) center form a chiral complex, high yield and high enantioselectivity are achieved, and a new way is provided for asymmetric synthesis of cyclobutane derivatives.

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Номер записи: 16
22-08-2023 дата публикации

Preparation method of isocyanate compound

Номер: CN116621736A
Автор: CHEN BIN, YAN PUCHA, LI YUANQIANG
Принадлежит:

The invention relates to a preparation method of an isocyanate compound, in particular to a preparation method of an aryl or heterocyclic isocyanate derivative. The isocyanate compound is prepared from an amine compound as a raw material through condensation and hydrolysis reactions. The process for preparing the benzyl isocyanate through the one-pot method is high in yield, low in raw material cost, short in reaction period, mild in reaction condition, environmentally friendly and capable of achieving industrial production.

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Номер записи: 17
08-08-2023 дата публикации

Preparation method of substituted sulfonic acid compound

Номер: CN116554067A
Автор: CHEN BIN, JIANG CHUNBO, YAN PUCHA, LI YUANQIANG, ZHANG YUNHAI
Принадлежит:

The invention relates to a preparation method of a substituted sulfonic acid compound, in particular to a preparation method of 2-fluoro-5-methanesulfonyl benzoic acid. 2-fluoro-5-halobenzoic acid and a derivative thereof are used as raw materials and are subjected to sulfonation reaction with a sulfonation reagent, and then alkylation reaction is further performed to prepare the compound shown in the formula I; the preparation method is high in yield, low in raw material cost, short in reaction period, mild in reaction condition, easy to operate and less in generated three wastes, and industrial production can be realized.

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Номер записи: 18
12-05-2023 дата публикации

Purification method of polypeptide easy to form hydrogel

Номер: CN116102614A
Автор: DENG DEXIONG, YU CHUAN, MA JIAQI, YAO WEIWEI, LI YUANQIANG, XU FENG
Принадлежит:

The invention provides a purification method of polypeptide easy to form hydrogel, which comprises the following steps: (1) dissolving a polypeptide crude product in a 30-60% acetic acid solution, and filtering to obtain a polypeptide crude product solution; (2) performing high performance liquid chromatography separation and purification on the polypeptide crude product solution to obtain a polypeptide eluent; and (3) adding acetic acid into the polypeptide eluent, distilling and concentrating to obtain the polypeptide. The purification method disclosed by the invention can be used for purifying most of gelatinous polypeptides, and a relatively good effect is achieved. The purity of the purified polypeptide reaches 99% or above, no tailing phenomenon exists, and the product yield is 50% or above.

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Номер записи: 19
23-06-2023 дата публикации

Asymmetric synthesis method of chiral cyclopropane derivative

Номер: CN116283660A
Автор: YAN PUCHA, ZHOU BO, HUA YUNYU, CHENG HOU'AN, SUN ZEBIN, FU XINGFENG, LI YUANQIANG
Принадлежит:

The invention provides an asymmetric synthesis method of a chiral cyclopropane derivative. Comprising the following steps: dissolving a compound 2 and an organic boride R-BXn in a solvent, and under the action of a catalyst, a ligand, an oxidant, an additive and alkali, obtaining the chiral cyclopropane derivative as shown in a formula 1, r'is selected from one of alkyl, alkoxy, aryl and substituted aryl, R is selected from one of alkyl, cycloalkyl and phenyl, X is selected from halogen, alkoxy or aryloxy, n is an integer of 1-3, and when n is 2 or 3, X can be the same or different. The method disclosed by the invention has a very broad-spectrum substrate application range and functional group compatibility, and has high selectivity and high yield; and the method is simple and is suitable for large-scale production and later modification of series medicines.

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Номер записи: 20
23-06-2023 дата публикации

Method for synthesizing N, 3, 3-trimethyl-2-oxobutanamide

Номер: CN116283635A
Автор: HUANG LIN, SHI CHANGGU, CHEN BIN, LI YUANQIANG
Принадлежит:

The invention provides a method for synthesizing N, 3, 3-trimethyl-2-oxobutyramide, which comprises the following steps of: synthesizing N, 3, 3-trimethyl-2-oxobutyramide; the method comprises the following steps: by taking 3, 3-dimethyl-2-oxobutyric acid as a raw material, carrying out condensation reaction on 3, 3-dimethyl-2-oxobutyric acid and methylamine hydrochloride under the action of organic alkali and a condensing agent to generate N, 3, 3-trimethyl-2-oxobutyramide. The yield of the N, 3, 3-trimethyl-2-oxobutanamide generated by the synthesis method is high and reaches 82%, the reaction condition is mild, the method is suitable for amplified production, high-toxicity raw materials are not adopted, and the method is safe and environmentally friendly.

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Номер записи: 21