796038-21-6Relevant articles and documents
Improved synthesis of capuramycin and its analogues
Wang, Yong,Siricilla, Shajila,Aleiwi, Bilal A.,Kurosu, Michio
, p. 13847 - 13858 (2013)
Capuramycin and its congeners are considered to be important lead molecules for the development of a new drug for multidrug-resistant (MDR) Mycobacterium tuberculosis infections. Extensive structure-activity relationship studies of capuramycin to improve the efficacy have been limited because of difficulties in selectively chemically modifying the desired position(s) of the natural product with biologically interesting functional groups. We have developed efficient syntheses of capuramycin and its analogues by using new protecting groups, derived from the chiral (chloro-4-methoxyphenyl)(chlorophenyl)methanols, for the uridine ureido nitrogen and primary alcohol. The chiral nonracemic (2,6-dichloro-4-methoxyphenyl)(2,4-dichlorophenyl)methanol derivative is a useful reagent to resolve rac-3-amino-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin- 2-one, the (S)-configuration isomer of which plays a significant role in improving the mycobactericidal activity of capuramycin. Battling TB: Capuramycin and its congeners (see scheme) are considered to be important lead molecules for the development of a new drug for multidrug-resistant Mycobacterium tuberculosis infections. Efficient synthesis of capuramycin and its analogues by using new protecting groups for the uridine ureido nitrogen and primary alcohol was accomplished. Copyright
PROCESSES FOR THE PREPARATION OF BENZODIAZEPINE DERIVATIVES
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Page/Page column 26-27, (2018/09/12)
The present invention relates to processes and intermediates useful in the preparation of biologically active molecules, especially in the synthesis of Respiratory Syncytial Virus (RSV) inhibitors. The present invention also relates to processes and intermediates for the preparation of compounds of formula (I). In particular, the present invention also relates to processes and intermediates for the preparation of compound (I-a).
PRODRUGS OF 1,4-BENZODIAZEPINONE COMPOUNDS
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Paragraph 00166, (2014/04/04)
Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R1 is H or CH3, and R2 is Ry; or b) R1 is Rx and R2 is H; wherein Rx and Ry are disclosed herein.