16851-56-2Relevant articles and documents
Preparation method and application of hydrazide indoles drugs
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Paragraph 0037; 0038; 0041, (2017/08/28)
The invention provides a preparation method and application of hydrazide indoles drugs, and discloses a 2-hydrazide substituted indole compound and a preparation method and application thereof. The novel 2-hydrazide substituted indole compound has quite high activity of inhibiting growth of tumor cells, and particularly has remarkable inhibiting effect on growth of human rectal cancer cells and colon cancer cells which have vascular endothelial growth factor receptor-2 subtype high expression; the IC50 value of the novel 2-hydrazide substituted indole compound can be about 10 mu M; the novel 2-hydrazide substituted indole compound has good antiangiogensis activity on a CAM (chick chorioallantoic membrane) model; and moreover, the compound 21 has good capability of resisting cell proliferation after HUVEC is stimulated by VEGF and specificity of resisting proliferation after HUVEC is simulated by VEGF.
Novel method for the synthesis of s-indoline-2- carboxylic acid and application thereof in the synthesis of perindopril
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Page/Page column 3, (2008/06/13)
Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): Application in the synthesis of perindopril and its pharmaceutically acceptable salts.
PROCESS AND PRODUCT
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Page 7; 22; scheme, (2010/02/09)
A process of preparing perindopril of formula (I), or a pharmaceutically acceptable salt thereof which process comprises protecting a compound of formula (II) where R denotes a hydrogen atom, in the presence of benzene sulphonic acid as a catalyst, to obtain the benzene sulphonic acid salt of an ester of formula (III) where Rl is a carboxyl protecting group and reacting said ester of formula (III) with N-[(S)-1-carbethoxybutyl]-(S)-alanine to obtain a compound of formula (IV) where Rl is as defined above; and deprotecting a compound of formula (IV) to yield perindopril of formula (I), or a pharmaceutically acceptable salt thereof. There is also provided by the present invention the benzene sulphonic acid salt of an ester of formula (III), and perindopril or a pharmaceutically acceptable salt thereof prepared by the above process.