БЕЛЫК Кевин М. (US),КЛИТОР Эдвард (GB),КО Шэнь-Чунь (US),МАЛИГРЕС Питер Эммануэль (US),СЯН Банпин (US),ЯСУДА Нобуеси (US),ИНЬ Цзяньго (US)
申请号：
RU2014141158
公开号：
RU2014141158A
申请日:
2013.03.13
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. A method of obtaining a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: X is selected from —C (R) = or —N =, where R is hydrogen, F or CN； Y is CH or N； R is selected from the group, consisting of C-alkyl, cyclopropylmethyl, cyclobutylmethyl and [1- (trifluoromethyl) cyclopropyl] methyl, each of which is optionally substituted by one or more substituents independently selected from the group consisting of F and hydroxy； and R 1 is hydrogen, methyl, F, Cl or Br； comprising initiating a reaction of a compound of formula F: wherein Ε is selected from the group consisting of halogen, —C (O) —OR ′ ′, —CN, —CONRR ′, —NRR ′, - CH-OR, OR, methyl and vinyl, wherein each of R and R ′ is independently selected from the group consisting of hydrogen, C-alkyl, aryl, heteroaryl or benzyl, and R ″ is hydrogen or a carbon-containing substituent capable of dissolving to a carboxylic acid, E represents a functional group with the ability to be a leaving group, and PG represents azo protecting group a, in the organic phase in the presence of a mono- or bis-quaternary salt of the quinch tree alkaloid and inorganic base in the aqueous phase, with the formation of a two-phase medium containing the aqueous phase and the organic phase, to obtain a compound of formula G: when Ε is different from -C (O) —O — H, substitution with a Carboxylic acid or conversion of an Ev carboxylic acid in a suitable chemical reaction to yield a compound of formula H: deprotection of a compound of formula H to yield a compound of formula C: optionally isolated as a salt, and binding of the compound of the forms ly C with a compound of formula V: optionally in salt form, under conditions to form an amide bond between the acid and amine to yield compounds of formula I.2. Way1. Способ получения соединения формулы I:или его фармацевтически приемлемой соли, где:X выбран из -C(R)= или -N=, где Rпредставляет собой водород, F или CN；Y представляет собой СН или N；Rвыбран из группы, сост
