Abstract: Novel crystalline hydrate form of (S)-1-phenylethylammonium (R)-diphenyl-methanesulphinyl-acetate and its use in a process for the preparation of (R)-benzhydrylsulphinylacetamide.
Type:
Grant
Filed:
November 4, 2008
Date of Patent:
June 5, 2012
Assignee:
Dipharma Francis S.R.L.
Inventors:
Giuseppe Barreca, Pietro Allegrini, Gabriele Razzetti
Abstract: The invention provides nitroaniline derivatives represented by general formula (I) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN, COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents.
Type:
Grant
Filed:
May 26, 1994
Date of Patent:
November 5, 1996
Assignee:
Cancer Research Campaign Technology Limited
Inventors:
William A. Denny, Brian D. Palmer, William R. Wilson
Abstract: A method is provided for preparing aromatic acetamides comprising reacting an aryl methyl ketone containing the same number of carbon atoms as the aromatic acetamide, with sulfur and ammonia under substantially anhydrous conditions. The method is particularly useful for the preparation of 4-hydroxyphenylacetamide from 4-hydroxyacetophenone.
Abstract: Described are D-(threo)-1-aryl-2-acylamido-3-fluoro-1-propanol esters and salts thereof, methods for their preparation, and methods for their use as antibacterial agents.