33465-36-0Relevant academic research and scientific papers
5,6,7,8-TETRAHYDRO[1,2,4]TRIAZOLO[4,3-a]PYRAZINE DERIVATIVES AS P2X7 MODULATORS
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Page/Page column 122-123, (2010/11/17)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6 R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.
ELECTROCHEMICAL S-S BOND FISSION OF 4-(2-BENZOTHIAZOLYLDITHIO)AZETIDINONES (KAMIYA'S DISULFIDES)
Torii, Sigeru,Tanaka, Hideo,Siroi, Takashi,Sasaoka, Michio,Saitoh, Norio,et al.
, p. 1829 - 1832 (2007/10/02)
An electrochemical S-S bond fission of 4-(2-benzothiazolyldithio)azetidinones derived from penicillin G has been achieved by the selection of an appropriate electrolysis system, providing either 2β-halomethylpenicillins, 3β-halocephams, or 4-methoxysulfinylazetidinone derivatives.
Process for preparing cephalosporins
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, (2008/06/13)
A process for preparing cephalosporins of structure: STR1 where R is hydrogen, C1 to C4 alkyl, cyano-methyl-, thienyl-methyl, furyl-methyl-, naphthyl-methyl-, phenyl-methyl-, phenoxy-methyl-, phenyl-isopropyl-, phenoxy-isopropyl-, pyridyl-4-thiomethyl-, and tetrazolyl-1-methyl; R1 is hydroxyl, C2 to C4 alkoxy, trichloroethoxy-, benzyloxy-, p-methoxy-benzyloxy-, p-nitrobenzyloxy-, benzhydryloxy-triphenylmethoxy-, phenacyloxy-, and p-halophenacyloxy; Z is hydrogen, hydroxyl, --O--alkyl, --O--CO--alkyl, --Br, --I, --N3, --NH2, --O--CO--CH3, --O--CO--NH2 and an --S--mononuclear nitrogen heterocyclic ring; Wherein a compound of structure STR2 is reacted in a suitable solvent at a temperature between -20° C and +80° C, in the presence of an aqueous organic or inorganic acid with an azoderivative of the formula: STR3 where R2 and R3 are equal or different and represent lower alkyl, a mononuclear aryl ring, CN--, a mononuclear heterocyclic ring, or the radicals --COR4, --COOR4, STR4 --CONHR4, or R2 and R3 together may represent the residues: STR5 where T represents >CH2, >N -- R4, and R4 is lower alkyl, a mononuclear aryl ring or a mononuclear heterocyclic ring, to give a compound of structure: STR6 in which R, R1, R2, R3, and Z have the meanings given above, and said intermediate (II 40 ) is reacted in a suitable solvent at a temperature between -100° C and +120° C with a compound selected from the class consisting of inorganic bases, to finally give the desired compound (III) which is isolated and purified in known manner.
