570416-36-3Relevant academic research and scientific papers
Synthesis of a CGRP Receptor Antagonist via an Asymmetric Synthesis of 3-Fluoro-4-aminopiperidine
Molinaro, Carmela,Phillips, Eric M.,Xiang, Bangping,Milczek, Erika,Shevlin, Michael,Balsells, Jaume,Ceglia, Scott,Chen, Jiahui,Chen, Lu,Chen, Qinghao,Fei, Zhongbo,Hoerrner, Scott,Qi, Ji,De Lera Ruiz, Manuel,Tan, Lushi,Wan, Baoqiang,Yin, Jingjun
, p. 8006 - 8018 (2019/06/17)
A practical and efficient enantioselective synthesis of the calcitonin gene-related peptide receptor antagonist 1 has been developed. The key structural component of the active pharmaceutical ingredient is a syn-1,2-amino-fluoropiperidine 4. Two approaches were developed to synthesize this important pharmacophore. Initially, Ru-catalyzed asymmetric hydrogenation of fluoride-substituted enamide 8 enabled the synthesis of sufficient quantities of compound 1 to support early preclinical studies. Subsequently, a novel, cost-effective route to this intermediate was developed utilizing a dynamic kinetic asymmetric transamination of ketone 9. This synthesis also features a robust Ullmann coupling to install a bis-aryl ether using a soluble Cu(I) catalyst. Finally, an enzymatic desymmetrization of meso-diester 7 was exploited for the construction of the γ-lactam moiety in 1.
2-BENZYLPYRIDAZINONE DERIVATIVES AS MET KINASE INHIBITORS
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Page/Page column 27-28, (2010/12/26)
Compounds of the formula I in which R1, R2, R3, R4′ have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
FUSED HETEROCYCLIC SULFONYLUREA COMPOUND, HERBICIDE CONTAINING THE SAME, AND METHOD OF CONTROLLING WEED WITH THE SAME
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Page 23, (2010/02/08)
The present invention provides a compound represented by the formula: wherein Q represents a fused heterocyclic group, X and Y are the same or different and each represent an optionally halogenated lower alkyl group, an optionally halogenated lower alkoxy group, etc. , or a salt thereof, as well as a herbicide comprising the compound or a salt thereof, which exhibits a significant effect for control of sulfonylurea herbicide-resistant weeds in paddy fields and can reduce the number of active ingredients in a combined preparation and a method of controlling sulfonylurea herbicide-resistant weeds which comprises using the same.
