4-AZIDOBUTYLAMINES AND PROCESSES FOR PREPARING

Neat 4-azidobutylamine and sails of 4-azidobutylamine and processes for producing the same are described herein. Amines represent a large class of organic compounds containing a basic nitrogen atom having a lone pair of electrons and one or more substituent groups. Many amines are used as precursors and feedstocks in a wide variety of industries such as textiles, agriculture, plastics, and pharmaceuticals. One such amine is 4-azidobutylamine, N3-(CH2)4NH2, an amine of butane that also includes an azide. 1. A process for preparing 4-azidobutylamine , the process comprising isolating the 4-azidobutylamine from a solvent that is substantially free or free of a chlorinated solvent.2. The process of wherein the solvent is N claim 1 , N-dimethyformamide or MTBE claim 1 , or a mixture thereof.3. The process of wherein the solvent is an aqueous solution.4. The process of further comprising raising the pH of the mixture.5. The process of further comprising separating an aqueous layer from the mixture.6. (canceled)7. Isolated 4-azidobutylamine substantially free of or free of a chlorinated solvent.8. An isolated salt of 4-azidobutylamine claim 4 , where the salt comprises a nitrate claim 4 , fluoride claim 4 , bromide claim 4 , iodide claim 4 , sulfate claim 4 , chlorosulfonate claim 4 , methanesulfonate claim 4 , toluenesulfonate claim 4 , phosphate claim 4 , phosphonate claim 4 , oxalate claim 4 , borate claim 4 , citrate claim 4 , malonate claim 4 , formate claim 4 , butyrate claim 4 , maleate claim 4 , propionate claim 4 , pyruvate claim 4 , benzoate claim 4 , or lactate claim 4 , or a combination thereof.910.-. (canceled)11. The salt of comprising an acid claim 8 , wherein the acid is selected from the group consisting of hydroiodide claim 8 , hydrobromide claim 8 , hydrofluoride claim 8 , nitric acid claim 8 , chlorosulfonic acid claim 8 , malonic acid claim 8 , formic acid claim 8 , butyric acid claim 8 , maleic acid claim 8 , propionic acid claim 8 , pyruvic acid ...

PROCESSES FOR PREPARING FLUOROKETOLIDES

Processes and intermediates for preparing fluoroketolide compounds are described herein. 2. The process of wherein the base is a cyclic amine base claim 1 , a non-aromatic amine base claim 1 , or an amine base with a conjugate acid pKa of at least about 11 claim 1 , or a combination of the foregoing.3. The process of wherein the base is sterically hindered.4. The process of wherein the base is a diamine.5. The process of wherein the base includes at least one nitrogen that does not have a hydrogen.6. The process of wherein the base includes at least one C=N group.7. The process of wherein the base is DBN or DBU claim 1 , or a combination thereof.8. The process of wherein the fluorinating agent is selected from the group consisting of NFSi claim 1 , Selectfluor claim 1 , and F-TEDA claim 1 , and combinations thereof11. The process of wherein the compound of formula (I) is solithromycin or a salt thereof.17. A composition comprising solithromycin that is substantially free of desfluoro solithromycin or N-desmethyl solithromycin claim 1 , or both.18. The composition of wherein the composition is substantially free of N desmethyl solithromycin.19. The composition of wherein the composition is substantially free of desfluoro solithromycin. This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application Ser. No. 62/129,305, filed Mar. 6, 2015, the disclosure of which is incorporated herein by reference.The invention described herein pertains to processes and intermediates for preparing fluoroketolide compounds.Fluoroketolide compounds have been reported to be highly effective in treating bacterial and protozoal infections. Moreover, fluoroketolide compounds have been reported to be particular effective in treating resistant bacterial and protozoal infections compared to corresponding non-fluoroketolides, macrolides, and azalides. However, reported manufacturing processes for ketolides proceed with low conversion, which leads to sometimes ...

PROCESSES FOR PREPARING FLUOROKETOLIDES

Processes and intermediates for preparing fluoroketolide compounds are described herein. 2. The process of wherein the amine base is a cyclic claim 1 , a non-aromatic amine base claim 1 , or a base with a conjugate acid pKa of at least about 11 claim 1 , at least about 11.5 claim 1 , at least about 12 claim 1 , at least about 12.5 claim 1 , or at least about 13 claim 1 , or a combination of the foregoing.3. The process of wherein the base is sterically hindered.4. The process of wherein the base is a diamine.5. The process of wherein the base includes at least one nitrogen that does not have a hydrogen.6. The process of wherein the base includes at least one C=N group.7. The process of wherein the base is DBN or DBU claim 1 , or a combination thereof.8. The process of any one of to wherein the fluorinating agent is selected from the group consisting of NFSi claim 1 , Selectfluor claim 1 , and F-TEDA claim 1 , and combinations thereof.11. The process of wherein the compound of formula (I) is solithromycin or a salt thereof.17. A composition comprising solithromycin that is substantially free of or free of desfluoro solithromycin.18. A composition comprising solithromycin that is substantially free of or free of N-desmethyl solithromycin. This application claims the benefit under 35 U.S.C. § 119(e) of U.S. Provisional Application Ser. No. 62/129,305, filed Mar. 6, 2015, the disclosure of which is incorporated herein by reference.The invention described herein pertains to processes and intermediates for preparing fluoroketolide compounds.Fluoroketolide compounds have been reported to be highly effective in treating bacterial and protozoal infections. Moreover, fluoroketolide compounds have been reported to be particular effective in treating resistant bacterial and protozoal infections compared to corresponding non-fluoroketolides, macrolides, and azalides. However, reported manufacturing processes for ketolides proceed with low conversion, which leads to sometimes ...

SYNTHESIS OF 1,4-DIAZASPIRO[5.5]UNDECAN-3-ONE

This invention provides a process for preparing 1,4-diazaspiro[5.5]undecan-3-one and analogues thereof that are useful in the preparation of pharmaceutical compound, including for the treatment of disorders involving abnormal cellular proliferation. Chemical intermediates in the process are also provided. 2. The process of claim 1 , wherein the nitroalkane is also a solvent.3. The process of claim 1 , wherein a base is used in step (a).4. The process of claim 3 , wherein the base is an organic base.5. The process of claim 3 , wherein the base is an inorganic base.6. The process of claim 1 , wherein oxalic acid is added after step (b) to precipitate and remove byproducts.7. The process of claim 1 , wherein an acid is added after step (b) to isolate the compound of Formula I as a salt.8. The process of claim 7 , wherein the acid is hydrobromic acid.9. The process of claim 1 , wherein Rand Rare hydrogen.10. The process of claim 9 , wherein Ris hydrogen.11. The process of claim 10 , wherein n is 1.12. The process of claim 11 , wherein y is 0.13. The process of claim 12 , wherein Ris —OMe or -OEt.16. The compound of claim 15 , wherein y is 1.17. The compound of claim 16 , wherein Ris halogen.18. The compound of claim 16 , wherein Ris alkyl.19. The compound of claim 15 , wherein Ris hydrogen.20. The compound of claim 19 , wherein n is 1.21. The compound of claim 20 , wherein y is 0.22. The compound of claim 21 , wherein Ris hydrogen.23. The compound of claim 22 , wherein Ris hydrogen.24. The compound of claim 23 , wherein Ris —OMe or -OEt. This application continuation of International Patent Application No. PCT/US2019/048029, filed in the U.S. Receiving Office on Aug. 23, 2019, which claims the benefit of provisional U.S. Application No. 62/722,675, filed Aug. 24, 2018. The entirety of each these applications is hereby incorporated by reference herein for all purposes.This invention provides a process for preparing 1,4-diazaspiro[5.5]undecan-3-one and analogues thereof ...

Lsd salt crystal forms

Polymorphic forms of lysergic acid diethyl amide (LSD) in crystalline salt forms. A pharmaceutical formulation of polymorphic forms of LSD in crystalline salt forms including pharmaceutically acceptable excipients. Polymorphic forms of LSD free-base. Polymorphic forms of a salt form of LSD.

Processes to prepare fluorocetolides

En la presente, se describen procesos e intermediarios para preparar compuestos de fluorocetólido. Here, processes and intermediates for preparing fluorocetolide compounds are described.

Processes for preparing fluoroketolides

Processes for preparing fluoroketolides

Processes and intermediates for preparing fluoroketolide compounds are described herein.

Microporous polyethylene hollow fibers and process for preparing them

ABSTRACT OF THE DISCLOSURE Normally hydrophobic, polyethylene hollow fibers having contiguous microporosity are prepared by extruding a melt of a polyethylene and an ester from a hollow fiber spinnerette, simultaneously cooling and drawing the forming fibers to a ratio of up to 40 to 1, drawing the gelled fibers to an overall ratio of from about 1.5/1 to 800/1 and then removing the ester. The maximum pore radius ranges up to about 50.ANG., and the fibers have gas permeabilities approaching 10-2 cc (STP) per cm2 per second per cm. Hg. transmembrane pressure differential. A significant increase in permeability over polyethylene hollow fibers made according to the teachings of the prior art is achieved.

HIV fusion inhibitor peptides with enhanced biological properties

Processes for preparing fluoroketolides

Processes and intermediates for preparing fluoroketolide compounds are described herein.

Hiv fusion inhibitor peptides with improved biological properties

Provided is an HIV fusion inhibitor peptide having an amino acid sequence of any one of SEQ ID NO:9. SEQ ID NO:10, SEQ ID NO:11, SEQ ID NO:12, SEQ ID NO:13, SEQ ID NO:14, or SEQ ID NO: 15; and provided is a pharmaceutical composition comprising a HIV fusion inhibitor peptide and one or more of a pharmaceutically acceptable carrier and macromolecular carrier, and uses and methods of treatment provided by these compositions.

PROCESSES TO PREPARE FLUOROCETOLIDES

En la presente, se describen procesos e intermediarios para preparar compuestos de fluorocetolido Herein, processes and intermediates for preparing fluoroketolide compounds are described.

Foam-core structure with graphics-imprinted skin

Synthesis of 1,4-diazaspiro[5.5]undecan-3-one

This invention provides a process for preparing 1,4-diazaspiro[5.5]undecan-3-one and analogues thereof that are useful in the preparation of pharmaceutical compound, including for the treatment of disorders involving abnormal cellular proliferation. Chemical intermediates in the process are also provided.

Methods of manufacture of r-mdma

A method of manufacturing R-MDMA by forming a Grignard reagent from 5-bromobenzodioxole, treating the Grignard reagent with S-propylene oxide to form chirally pure alcohol 1, activating the alcohol as mesylate 2, converting to chirally pure azide 3, reducing the azide to amine 4, protecting the amine with di-tert-butyl dicarbonate, reducing the protected amine 5 to yield R-MDMA free base 6, and treating with an acid to form a salt 7 in >99% e.e. A method of manufacturing S-MDMA by forming a Grignard reagent from 5-bromobenzodioxole, treating the Grignard reagent with R-propylene oxide to form chirally pure alcohol 8, activating the alcohol as mesylate 9, converting to chirally pure azide 10, reducing the azide to amine 11, protecting the amine with di-tert-butyl dicarbonate, reducing the protected amine 12 to yield S-MDMA free base 13, and treating with an acid to form a salt 14 in >99% e.e.

18-mc salt forms

A composition including a salt of 18-MC, wherein the salt is chosen from gentisate, hydrobromide, besylate, napadisylate, hydrochloride, sulfate, oxalate, maleate, mesylate, and tosylate. A composition including a polymorph of 18-MC.

Lsd salt crystal forms

Polymorphic forms of lysergic acid diethyl amide (LSD) in crystalline salt forms. A pharmaceutical formulation of polymorphic forms of LSD in crystalline salt forms including pharmaceutically acceptable excipients. Polymorphic forms of LSD free-base. Polymorphic forms of a salt form of LSD.

Lsd salt crystal forms

Polymorphic forms of lysergic acid diethyl amide (LSD) in crystalline salt forms. A pharmaceutical formulation of polymorphic forms of LSD in crystalline salt forms including pharmaceutically acceptable excipients. Polymorphic forms of LSD free-base. Polymorphic forms of a salt form of LSD.

18-mc salt forms

A composition including a salt of 18-MC, wherein the salt is chosen from gentisate, hydrobromide, besylate, napadisylate, hydrochloride, sulfate, oxalate, maleate, mesylate, and tosylate. A composition including a polymorph of 18-MC.

R-mdma crystal forms

A composition of a crystalline form salt or polymorph of R-MDMA. A pharmaceutical composition of a crystalline form salt or polymorph of R-MDMA and pharmaceutically acceptable excipients. A method of treating an individual for a medical condition, by administering an effective amount of a composition of a crystalline form salt or polymorph of R-MDMA to the individual and treating the individual.

18-mc salt forms

A composition including a salt of 18-methoxycoronaridine (18-MC), wherein the salt is chosen from hydrobromide, besylate, napadisylate, hydrochloride, sulfate, oxalate, maleate, mesylate, and tosylate salts, more preferably a gentisate salt. Furthermore, a composition including a polymorph of a salt of 18-MC, characterized by its X-ray Powder Diffraction pattern and its endothermic signal from Differential Scanning Calorimetry.

Lsd salt crystal forms

Polymorphic forms of lysergic acid diethyl amide (LSD) in crystalline salt forms. A pharmaceutical formulation of polymorphic forms of LSD in crystalline salt forms including pharmaceutically acceptable excipients. Polymorphic forms of LSD free-base. Polymorphic forms of a salt form of LSD.

Lsd salt crystal forms

Retractable water board fin

Methods of synthesis for therapeuthic anti-hiv peptides

Provided herein are methods for synthesis of peptides. In particular, provided herein are methods of synthesis for therapeutic antiviral peptides.

Synthesis of 1,4-Diazaspiro[5.5]Undecan-3-One

This invention provides a process for preparing 1,4-diazaspiro[5.5]undecan-3-one and analogues thereof that are useful in the preparation of pharmaceutical compound, including for the treatment of disorders involving abnormal cellular proliferation. Chemical intermediates in the process are also provided.

Recreational water slide/play pool