40216-82-8Relevant articles and documents
Novel chiral derivatizing agents for 1H NMR determination of enantiomeric purities of carboxylic acids
Wada, Koji,Goto, Mizuko,Yamashita, Hiroshi,Nagasawa, Kazuo
, p. 964 - 978 (2017/06/13)
(S)-4-(3-Aminopyrrolidin-1-yl)coumarin (1), (S)-4-(3-aminopiperidin-1-yl)coumarin (4), and (S)-4-(3-aminoazepan-1-yl)coumarin (7), prepared from 4-chlorocoumarin and (S)-pyrrolidin-3-amine, (S)-piperidin-3-amine, and (S)-azepan-3-amine, respectively, were proven to be versatile and reliable 1H NMR optical purity determination agents for chiral carboxylic acids.
Development of a large-scale synthesis of sulphostin, a dipeptidyl peptidase IV inhibitor
Abe, Masatoshi,Nagai, Masashi,Yamamoto, Keiichiro,Yamazaki, Hiroko,Koga, Ichiro,Satoh, Yoshitaka,Muraoka, Yasuhiko,Kurashige, Shuji,Ichikawa, Yuh-Ichiro
, p. 570 - 576 (2012/12/25)
For the progress of the in vivo study on sulphostin, a dipeptidyl peptidase IV inhibitor, its large-scale synthetic method was investigated. The optical resolution of (3S,RSP)-1-amino(sulfoamino)phosphinyl-3- benzyloxycarbonylamino-2-piperidinone, which was the most difficult step in the previous method, was simplified by using fractional crystallization. The use of 2 mol equiv of (1S,2R)-(+)-2-amino-1,2-diphenylethanol for optical resolution gave desired diastereomer 15 in good yield as a less soluble salt. In the present synthetic method, there were no requirements for purification using column chromatography, reaction at cryogenic temperature, and treatment using the haloalkane solvents. The total yield of the new method was 4.6%, which was an improvement of approximately 2-fold compared to the method reported previously.
NEW HETEROCYCLIC AMIDE COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
-
Page 49, (2010/11/30)
The present invention relates to novel heterocyclic compounds that inhibit phosphodiesterase type 4 (PDE 4). The compounds are useful for treating inflammatory conditions, diseases of the central nervous systems and insulin resistant diabetes.