120658-70-0Relevant articles and documents
Preparation method of cinacalcet hydrochloride
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Paragraph 0029; 0039-0040, (2020/10/05)
The invention relates to a preparation method of cinacalcet hydrochloride. The preparation method comprises the following steps: taking m-trifluoromethyl benzaldehyde, hydantoin and (R)-1-(1-naphthyl)ethylamine as raw materials, performing condensation, hydrolysis, amidation and reduction reaction to prepare cinacalcet, and reacting cinacalcet with hydrochloric acid to prepare cinacalcet hydrochloride. Compared with an existing synthesis method of cinacalcet hydrochloride, the preparation method is short in route and low in raw material cost, the adopted condensing agent is oxalyl chloride and thionyl chloride, which are low in price, the adopted reducing agent is sodium borohydride, which is low in price, a precious metal catalyst (palladium on carbon) is not used, the hydrogenation reaction step is avoided, the requirement for equipment is low, normal-pressure reaction operation can be adopted, and the method is suitable for large-scale industrial production.
2-OXO-1,2,4,5-TETRAHYDRO-1,3-BENZODIAZEPIN-3-YL-PIPERIDINES USED AS CGRP ANTAGONISTS
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Page/Page column 73-74, (2010/11/24)
The invention relates to novel CGRP antagonists of general formula (I), in which B, R1 and R2 are defined as cited in claim 1, to their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts, in addition to the hydrates of their salts, in particular their physiologically compatible salts, with inorganic or organic acids or bases. The invention also relates to medicaments containing said compounds, to their use and to a method for their production.
Synthesis and activity of novel analogs of hemiasterlin as inhibitors of tubulin polymerization: Modification of the a segment
Yamashita, Ayako,Norton, Emily B.,Kaplan, Joshua A.,Niu, Chuan,Loganzo, Frank,Hernandez, Richard,Beyer, Carl F.,Annable, Tami,Musto, Sylvia,Discafani, Carolyn,Zask, Arie,Ayral-Kaloustian, Semiramis
, p. 5317 - 5322 (2007/10/03)
Analogs of HTI-286 (1), containing various aromatic rings in the A segment, were synthesized as potential inhibitors of tubulin polymerization, and the structure-activity relationships related to stereo- and regio-chemical effects of substituents on the a