90802-45-2Relevant articles and documents
Preparation method of lenadomide
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, (2019/06/07)
The invention discloses a preparation method of lenalidomide, and belongs to the field of organic synthesis. 2-methyl-3-methyl nitrobenzoate and 3-N-benzyloxy-carbonyl-L-glutamine serve as starting materials, and an important intermediate 2-brooethyl-3-methyl nitrobenzoate is obtained through a bromination reaction of 2-methyl-3-methyl nitrobenzoate. 3-N-benzyloxy-carbonyl-L-glutamine is cyclizedunder catalysis to produce 3-N-benzyloxy-carbonyl-2,6-dioxopiperidine, an amino group is subjected to deprotection to produce 3-amino-2,6-piperidone halide, 3-(4-nitro-1-oxo-1,3-o-xylylenimine-2-yl)piperidine-2,6-diketone is obtained through an aminolysis reaction of 3-N-benzyloxy-carbonyl-2,6-dioxopiperidine and 2-brooethyl-3-methyl nitrobenzoate, and then lenalidomide is prepared through reduction. The method has the advantages that the cost of raw materials are low, aftertreatment is simple, and the yield is high, and the production cost of the lenalidomide as a bulk drug is greatly reduced. The method is a convenient and efficient lenalidomide synthesis method suitable for industrial production.
Hydrolyzed metabolites of thalidomide: Synthesis and TNF-α production-inhibitory activity
Nakamura, Takanori,Noguchi, Tomomi,Miyachi, Hiroyuki,Hashimoto, Yuichi
, p. 651 - 654 (2008/02/08)
Putative hydrolyzed metabolites of thalidomide were prepared and characterized, and their inhibitory activity on tumor necrosis factor (TNF)-α production in the human monocytic leukemia cell line THP-1 was evaluated. α-(2-Carboxybenzamido)glutarimide was a more potent TNF-α production inhibitor than thalidomide.
Studies towards the synthesis of the benzodiazepine alkaloid auranthine. Synthesis of an acetylated derivative
Witt, Anette,Gustavsson, Annika,Bergman, Jan
, p. 29 - 35 (2007/10/03)
Different approaches towards the synthesis of auranthine have been investigated. A completed synthesis of 3-[2-(4-oxo-3,4-dihydro-quinazolin-2-yl)- ethyl]-3,4-dihydro-1H-benzo[e][1,4]-diazepine-2,5-dione, an auranthine precursor, which after dehydration w