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1. RU0002666731 - METHOD FOR PRODUCING OPTICALLY ACTIVE ENANTIOMERS OF PIRLINDOLE AND ITS SALTS

Office Russian Federation
Application Number 2016148181
Application Date 09.05.2014
Publication Number 0002666731
Publication Date 12.09.2018
Grant Number
Grant Date 12.09.2018
Publication Kind C2
IPC
A61K 31/495
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
C07D 487/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
06Peri-condensed systems
CPC
C07B 57/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
57Separation of optically-active compounds
C07D 487/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
06Peri-condensed systems
C07B 2200/07
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
07Optical isomers
A61K 31/495
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
C07D 487/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by C07D451/00 - C07D477/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Inventors ПАРДАЛ ФИЛИПИ Аугушту Эужениу (PT)
ЭУФРАЗИУ ПЕДРОЗУ Педру Филипи (PT)
АЛМЕЙДА ПЕКОРЕЛЛИ Сузана Маркеш (PT)
КАЗИМИРУ КАИШАДУ Карлош Алберту Эуфразиу (PT)
ЛОПЕШ Ана София да Консейсау (PT)
ДАМИЛ Жоан Карлош Рамош (PT)
Э ОЛИВЕЙРА САНТОШ Педру Паулу ди Ласерда (PT)
PARDAL FILIPE, Augusto Eugenio (PT)
EUFRASIO PEDROSO, Pedro Filipe (PT)
ALMEIDA PECORELLI, Susana Marques (PT)
CASIMIRO CAIXADO, Carlos Alberto Eufrasio (PT)
LOPES, Ana Sofia da Conceicao (PT)
DAMIL, Joao Carlos Ramos (PT)
E OLIVEIRA SANTOS, Pedro Paulo de Lacerda (PT)
Title
(EN) METHOD FOR PRODUCING OPTICALLY ACTIVE ENANTIOMERS OF PIRLINDOLE AND ITS SALTS
(RU) СПОСОБ ПОЛУЧЕНИЯ ОПТИЧЕСКИ АКТИВНЫХ ЭНАНТИОМЕРОВ ПИРЛИНДОЛА И ЕГО СОЛЕЙ
Abstract
(EN)
FIELD: chemistry. SUBSTANCE: invention relates to a novel process for the preparation of optically active enantiomers of pirlindole selected from the group consisting of enantiomerically pure (S)-pirlindole and (R)-pirlindole, in free base form or in the form of a pharmaceutically acceptable salt, characterized in that separation by crystallization with optically active acids (rac)-pirlindole in the form of a free base is carried out, wherein the optically active acids are selected from the group consisting of: (R)-mandelic acid, (R)-(+)-α-methoxy-α-trifluoromethylphenylacetic acid and (S)-mandelic acid. EFFECT: new method for the preparation of optically active enantiomers of pyrrolindole, which is a reversible inhibitor of monoamine oxidase A, can be used to treat depression. 14 cl, 12 ex

(RU)
Изобретение относится к новому способу получения оптически активных энантиомеров пирлиндола, выбранных из группы, состоящей из энантиомерно чистых (S)-пирлиндола и (R)-пирлиндола, в форме свободного основания или в форме фармацевтически приемлемой соли, отличающийся тем, что проводят разделение путем кристаллизации с оптически активными кислотами (рац)-пирлиндола в форме свободного основания, где оптически активные кислоты выбраны из группы, состоящей из: (R)-миндальной кислоты, (R)-(+)-α-метокси-α-трифторметилфенилуксусной кислоты и (S)-миндальной кислоты. Технический результат: разработан новый способ получения оптически активных энантиомеров пирлиндола, который является обратимым ингибитором моноаминооксидазы А и может применяться для лечения депрессии. 13 з.п. ф-лы, 12 пр.

Also published as
CL2016-2843
CN201480078731.6
CONC2016/0003926
GE14340
GE14340/1
IR139550140003010460
KZ2016/1150.1
MA39449
SA516380265
UAa201611334