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1. CN101679420 - A method for the preparation of an enantiomerically pure benzazepine

Office
China
Application Number 200880016528.0
Application Date 10.04.2008
Publication Number 101679420
Publication Date 24.03.2010
Grant Number 101679420
Grant Date 14.05.2014
Publication Kind B
IPC
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
CPC
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 471/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
12in which the condensed system contains three hetero rings
14Ortho-condensed systems
Applicants 默沙东有限责任公司
Inventors J·P·G·希尔丹
G·J·坎珀曼
Agents 中国国际贸易促进委员会专利商标事务所 11038
Priority Data 07105979.4 11.04.2007 EP
Title
(EN) A method for the preparation of an enantiomerically pure benzazepine
(ZH) 一种制备对映体纯的苯并氮杂*的方法
Abstract
(EN) The invention relates to a method for the preparation of a cyclic compound according to formula (III) comprising reacting a compound according to Formula (I) and a compound according to formula (II),wherein in Formula (I), R1, R2, R3 and R4 may be hydrogen or substituent groups comprising one or more carbon atoms and/or hetero-atoms, wherein R1, R2, R3 and R4 can be combined in aromatic or aliphatic ring structures, -Y is a ring element comprising 1-3 substituted or unsubstituted carbon atoms and/or heteroatoms in the ring and -R5 is hydrogen or a hydrocarbon substituent group comprising oneor more carbon atoms and optionally one or more hetero atoms, and wherein in Formula (II), Z1 and Z2 are, leaving groups, X is a reactive functional hydrocarbon group for subsequent ring closure, comprising one or more carbon atoms and a reactive functional group and having a chain of between 1 to 6 atoms between the carbon atom attached to the central carbon atom of formula (II) and the reactivefunctional group and R8 is hydrogen or a hydrocarbon substituent different from X making the central carbon atom of formula II a chiral centre in Formula (III) and wherein reactive functional group Xcan be or can be extended to be compound of formula (IV) which can be ring closed to produce the polycyclic component of formula (V). More in particular, the invention relates to the preparation of mirtazapine precursors and mirtazapine preferably having a substantial enantiomeric excess.
(ZH)

本发明涉及制备式III的环状化合物的方法,该方法包括使式I的化合物和式II的化合物反应,其中在式I中,R1、R2、R3和R4可以是氢或包含一个或多个碳原子和/或杂原子的取代基,其中R1、R2、R3和R4可以结合在芳族或脂肪族环结构中,-Y是包含环中的1-3取代或未取代的碳原子和/或杂原子的环成分,和-R5是氢或包含一个或多个碳原子和任选地包含一个或多个杂原子的烃取代基,并且其中在式II中,Z1和Z2是离去基团,X是用于随后的环闭合的反应性官能烃基,其包含一个或多个碳原子和反应性官能团,并且在连接到式II的中心碳原子的碳原子和所述反应性官能团间具有1-6原子的链,并且R8是氢或不同于X的、使得式II的中心碳原子成为式III中的手性中心的烃取代基,并且其中反应性官能团X可以是或可以被扩展成式IV的化合物,其可以被闭环以产生式V的多环成分。更特别地,本发明涉及优选具有显著的对映体过量的米氮平前体和米氮平的制备。