Title:
【発明の名称】レチン酸様活性を有するジ置換アセチレンを製造するための方法および中間体
Document Type and Number:
Japanese Patent JP3055794
Kind Code:
B2
Abstract:
A process is disclosed for the preparation of disubstituted acetylene derivatives having retinoic acid like biological activity, wherein 6-ethynyl-chroman, 6-ethynyl-thio chroman and 6-ethynyl-1,2,3,4-tetrahydroquinoline derivatives of the formula shown below are reacted in the presence of catalysts with halogenated phenyl or heteroaryl derivatives of the formula shown below to provide the disubstituted acetylenes. In the formulae the symbols have the following meanings, R1, R2, R3, R4 and R5 are hydrogen or lower alkyl groups (of 1-6 carbons) where R1, R2, R3, R4 and R5 may be identical or different from one another) X is S, O or NR min where R min is hydrogen or lower alkyl, Z represents hydrogen, or a metal ion capable of forming a salt with the ethynyl moiety of the molecule, X min is a leaving group such as a halogeno group, A is phenyl, or heteroaryl such as pyridinyl, thienyl, furyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl or oxazolyl, n is an intetger between 0 to 5, and B is H, -COOH or a pharmaceutically acceptable salt, ester or amide thereof, -CH2OH or an ether or ester derivative, or -CHO or an acetal derivative, or -COR1 or a ketal derivative where R1 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons. u
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Inventors:
Roshanta AS Chandra Ratna
Application Number:
JP25166090A
Publication Date:
June 26, 2000
Filing Date:
September 19, 1990
Export Citation:
Assignee:
Allergan, Incorporated
International Classes:
A61K31/185; A61K31/353; A61K31/38; A61K31/382; A61K31/41; A61K31/44; A61K31/4427; A61K31/443; A61K31/4433; A61K31/445; A61K31/47; A61P17/00; A61P27/02; A61P29/00; A61P35/00; A61P37/06; A61K31/135; A61P43/00; B01J27/122; B01J27/185; B01J31/22; C07B61/00; C07D215/06; C07D215/12; C07D215/14; C07D311/04; C07D311/20; C07D311/58; C07D333/54; C07D335/06; C07D401/06; C07D405/06; C07D407/06; C07D409/06; C07D413/06; C07D417/06; (IPC1-7): C07D215/06; B01J27/122; B01J27/185; B01J31/22; C07D215/12; C07D311/04; C07D311/58; C07D335/06; C07D401/06; C07D405/06; C07D407/06; C07D409/06; C07D413/06; C07D417/06
Domestic Patent References:
| JP63255277A | ||||
| JP3120273A |
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)