PREPARATION OF 2S,3S-N-ISOBUTYL-N-(2- HYDROXY-3-AMINO-4-PHENYLBUTYL)-P- NITROBENZENESULFONYLAMIDE HYDROCHLORIDE AND OTHER DERIVATIVES OF 2-HYDROXY-l,3- DIAMINES
ثبت نشده
چکیده
The present invention provides a new process for the preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2S,3S-N-isobutyl-N-(2hydroxy -3 -amino -4-phenylbu tyl) -pnitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present invention can be used to prepare not only the 2S,3S-derivative, but also the 2R,3S-, 2S,2Rand the 2R,3R-derivatives. (57) 27 Claims, 1 Drawing Sheet Related U.S. Application Data US 2003/0181723 A1 Sep. 25, 2003 Appl. No.: 10/382,185
منابع مشابه
PREPARATION OF 2S,3S-N-ISOBUTYL-N-(2- HYDROXY-3-AMINO-4-PHENYLBUTYL) -P- NITROBENZENESULFONYLAMIDE HYDROCHLORIDE AND OTHER DERIVATIVES OF 2-HYDROXY-l,3- DIAMINES
Inventors: Aslam A. Malik, Cameron Park, CA (US); Hasan Palandoken, Woodland, CA (US); Joy A. Stringer, Carmichael, CA (US); Roland P. Carlson, Folsom, CA (US); John Leach, Gold River, CA (US); Thomas G. Archibald, Fair Oaks, CA (US); Robert G. Miotke, Gold River, CA (US) PREPARATION OF 2S,3S-N-ISOBUTYL-N-(2HYDROXY-3-AMINO-4-PHENYLBUTYL) -PNITROBENZENESULFONYLAMIDE HYDROCHLORIDE AND OTHER DERIV...
متن کاملFunctional and molecular characterization of beta-adrenoceptors in the internal anal sphincter.
The purpose of the present study was to characterize different beta-adrenoceptors (beta-ARs) and determine their role in the spontaneously tonic smooth muscle of the internal anal sphincter (IAS). The beta-AR subtypes in the opossum IAS were investigated by functional in vitro, radioligand binding, Western blot, and reverse transcription-polymerase chain reaction (RT-PCR) studies. ZD 7114 [(S)-...
متن کاملEnzymatic deacetylation of N-hydroxy-2-acetylaminofluorene by liver microsomes.
Af-Hydroxy-2-acetylaminofluorene was rapidly deacetylated by guinea pig liver and, to a lesser extent, by other guinea pig tissues examined. The enzyme activity was located in the microsomal fraction of the liver. The enzyme appeared to be stimulated by trisodium pentacyanoamine ferrate, and it was inhibited by SKF-525A (|3-diethylaminoethyldiphenylpropyl acetate hydrochloride), by sodium fluor...
متن کاملThe CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor.
4-{[4-({(3R)-1-Butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenyl]oxy}benzoic acid hydrochloride (873140) is a potent noncompetitive allosteric antagonist of the CCR5 receptor (pK(B) = 8.6 +/- 0.07; 95% CI, 8.5 to 8.8) with concomitantly potent antiviral effects for HIV-1. In this article, the receptor-based mechanism of action of 873140 is compared ...
متن کاملCytokinins : Synthesis and Biological Activity of Geometric and Position Isomers of
Geometric and position isomers of zeatin and of ribosylzeatin and other compounds closely related to zeatin have been tested in the tobacco (Nicotiana tabacum var. Wisconsin No. 38) bioassay. None was more active than zeatin itself. There was a much greater difference in activity (> 50-fold) between transand cis-zeatin than between trans-isozeatin [6(4-hydroxy-2-methyl-trans-2-butenylamino)puri...
متن کامل