131150-36-2Relevant academic research and scientific papers
Preparation method of carfilzomib intermediate and intermediate chemical compounds of carfilzomib
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Paragraph 0059; 0060; 0061; 0062, (2016/10/07)
The invention discloses a novel preparation method of a carfilzomib key intermediate. L-leucine is taken as an original raw material, two reactive hydrogen on an amino group are protected, a chemical compound V is prepared and subjected to Weinreb amidation, a chemical compound IV is prepared, IV and 2-allyl magnesium bromide have a reaction, a chemical compound III is prepared and has an epoxidation reaction, a chemical compound II is prepared and subjected to deamination protection, and a chemical compound I is prepared. The invention further discloses intermediate chemical compounds II, III, IV and V of carfilzomib. The preparation method is simple to operate, the total yield is high, the cost is low, the selectivity is high, and the preparation method is suitable for industrial production.
Stereoselective total synthesis of amicoumacin C
Suzuki, Tomomi,Nagasawa, Tomohiro,Enomoto, Masaru,Kuwahara, Shigefumi
, p. 1992 - 1997 (2015/04/21)
The enantio- and diastereoselective total synthesis of amicoumacin C was achieved from l-phenylalanine in 17% overall yield through 13 steps via condensation between an amine and an acid segment. The amine segment was prepared from l-leucine in 42% yield
