75130-29-9Relevant articles and documents
Preparation method of hypotensive drug (R)-cilnidipine
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Paragraph 0021; 0029-0034, (2018/04/26)
The invention relates to the preparation field of a single configuration of a hypotensive drug (R)-cilnidipine, in particular to a preparation method of a hypotensive drug (R)-cilnidipine. The preparation method comprises the following steps: 1) adding ethyl cyano acetoacetate, m-nitrobenzaldehyde, 3-amino-2-methoxyethyl butenoate into isopropanol for a reflux reaction to obtain a racemized product; 2) adding the racemized product into an aqueous solution, adding lipase as a catalyst to stir for a catalytic reaction, and after reaction, acidifying and filtering a reaction liquid to obtain (R)-1,4-dihydrogen-2,6-dimethyl-4-(3-nitryl phenyl)-3,5-dipicolinic acid-5-(2-methoxyl ethyl); and 3) carrying out an esterification reaction with cinnamyl alcohol to obtain (R)-cilnidipine. The method provided by the invention obtains (R)-cilnidipine with high selectivity and high yield, and ee% reaches up to 99.7%.
Synthesis and antihypertensive activities of new 1,4-dihydropyridine derivatives containing a nitrooxy moiety at the 3-ester position
Ogawa,Nakato,Tsuchida,Hatayama
, p. 108 - 116 (2007/10/02)
The synthesis of a new series of dihydropyridines containing a nitrooxy moiety at the 3-ester position is described. The antihypertensive activity of the compounds was examined and compared with that of nifedipine; some of them were relatively potent. The structure-activity relationship is also discussed.