New piperidine derivatives and processes for preparing the same
Номер патента: GB963639A
Опубликовано: 15-07-1964
Автор(ы): Alma Beryl Simmonds, Arnold Heyworth Beckett, Norman James Harper
Принадлежит: Individual
Опубликовано: 15-07-1964
Автор(ы): Alma Beryl Simmonds, Arnold Heyworth Beckett, Norman James Harper
Принадлежит: Individual
Реферат: The invention comprises compounds of the general formula: <FORM:0963639/C1/1> and pharmaceutically acceptable acid addition salts thereof, wherein R1 is a hydrogen atom or a G-3-alkanoyl group; R2 is a hydrogen atom or a G-3 alkyl group; R3 is a phenyl group optionally substituted by a halogen atom or an alkyl group, or a 21-thienyl group optionally substituted by an alkyl group; R4 is a benzyl group substituted by one or more halogen atoms and n is 2, 3 or 4 and their preparation by reacting a compound of the general formula: <FORM:0963639/C1/2> with a compound X-(CH2)nCOR3 where X is a halogen atom in the presence of an alkali-metal bicarbonate and an alkali-metal iodide to give a compound where R1 is a hydrogen atom or with the methiodide of (CH3)2N(CH2)2COR3 in the presence of dimethyl formamide and an alkali metal carbonate or with formaldehyde and a ketone CH3COR3 to give a compound where R1 is a hydrogen atom and n is 2 or by reacting an aminoalkohol of the formula: <FORM:0963639/C1/3> with a mixture of an alkanoic anhydride and an organic base. Salts formed as products may be converted into their bases and bases into their acid addition salts. 4-(41-Chlorobenzyl)-4-piperidinol and its hydrochloride was prepared by reacting N-benzylpiperidone with 4-chlorobenzyl magnesium chloride to give N-benzyl-4-(41-chlorobenzyl)-4-piperidinol and hydrogenolysing the latter. Similarly were prepared 4-(31141-dichlorobenzyl) -and -(211 41-dichlorobenzyl)-4-piperidinols and their N-benzyl analogues.
Processes for preparing (3r,4r)-1-benzyl-n,4-dimethylpiperidin-3-amine or a salt thereof and processes for preparing tofacitinib using the same
Номер патента: EP3927689A1. Автор: Ji-hye CHOI,Sung-Hee Cho,Sang-Won Kim,Doo-Byung Lee,Sang-Ho Oh,Su-Young Lee,Kyoung-Chan Kwon,Hyo-Ick HWANG,Kyeong-Sill LEE,Ik-Su JO. Владелец: Yuhan Corp . Дата публикации: 2021-12-29.