81403-67-0Relevant articles and documents
Improved method used for preparing quinazoline drugs
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Paragraph 0032; 0039; 0055; 0056, (2018/07/06)
The invention relates to an improved method used for preparing quinazoline drugs, and provides a synthesis route taking 2-chloro-4-amino-6,7-dimethoxyquinazoline as an intermediate. The synthesis route comprises following steps: acrylonitrile and a methylamine alcohol solution are subjected to amination reaction so as to obtain intermediate (I); triethylamine is taken as an acid binding agent, andbenzyl chloride is taken as a protective group so as to obtain an intermediate (II); a metal hydride is adopted so as to obtain an intermediate (III) through reduction; acylation with tetrahydro-2-furancarbonylchloride is carried out so as to obtain an intermediate (IV); the intermediate (IV) and ammonium formate are subjected to hydrogenolysis under catalytic effect of palladium on carbon so asto obtain an intermediate (V); and at least condensation reaction with 2-chloro-4-amino-6,7-dimethoxyquinazoline is carried out so as to obtain quinazoline drug Alfuzosin Hydrochloride (VI). Comparedwith the prior art, the improved method possesses following advantages: operation is simple and safe; reaction conditions are convenient to control; energy consumption is low; yield is stable; and industrialized application prospect is promising.
Chemoselective calcium-catalysed direct amidation of carboxylic esters
Nguyen, D. Thao,Lenstra, Danny C.,Mecinovi?, Jasmin
, p. 77658 - 77661 (2015/09/28)
Unactivated carboxylic esters and primary amines undergo calcium-catalysed direct amide bond formation in excellent yields under homogeneous conditions in toluene. This green and mild reaction proceeds chemoselectively with esters, whereas related carboxylic acids and amides remain unreactive.
AN IMPROVED AND INDUSTRIAL PROCESS FOR THE PREPARATION OF ALFUZOSIN HYDROCHLORIDE AND ITS NOVEL POLYMORPHS
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Page/Page column 11, (2008/06/13)
An improved and industrial process for the preparation of Alfuzosin Hydrochloride and its novel polymorphs (Formula (I)).