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.
NEW PROCESSES FOR THE PREPARATION OF OPTICALLY PURE INDOLINE-2-CARBOXYLIC ACID AND N-ACETYL-INDOLINE-2-CARBOXYLIC ACID
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Page/Page column 16-17, (2008/06/13)
Processes for: a) separating the enantiomers of indoline-2-carboxylic acid of formula (I): comprising of: (i) combining the (R, S) indoline-2-carboxylic acid with (1S)- or (1R)-10- camphorsulfonic acid as the resolving agent in a resolution solvent and crystallizing from the said mixture the diastereomeric salt of (S)- or (R)-indoline-2-carboxylic acid with optically pure (1S)- or (1R)-10-camphorsulfonic acid; (ii) regenerating the (S)- or (R)-indoline-2-carboxylic acid from the crystallized diastereomeric salt by using a suitable base or basic ion-exchange resin; and b) for the optical resolution of N-acetyl-indoline-2-carboxylic acid of formula, (II): comprising of: (i) combining the (R, S)-N-acetyl-indoline-2-carboxylic acid with (S)- or (R)- phenylglycinol as the resolving agent in a resolution solvent and crystallizing from the said mixture the diastereomeric salt of (S)- or (R)-N-acetyl-indoline-2-carboxylic acid with optically pure phenylglycinol; (ii) regenerating the (S)- or (R)-N-acetyl-indoline-2-carboxylic acid from the crystallized salt by using a suitable acid or acidic ion-exchange resin. The non-selected enantiomer may then be racemized and the process (a) or (b) repeated thus to obtain substantial conversion of the material to one enantiomer.
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.