PRODUCING INDAN DERIVATIVES PRODUCING INDAN DERIVATIVES

摘要

1375170 Indonecarboxylic acid derivatives TAKEDA YAKUHIN KOGYO KK 23 Dec 1971 [29 Dec 1970 6 May 1971] 60022/71 Heading C2C The invention comprises compounds of formula and their alkyl esters, amides and metal salts, wherein RSP1/SP is H or halogen, and a process for making them by reducing the corresponding oxocyclohexyl analogues (A), optionally followed (where RSP1/SP = H in the product) by halogenation. Other exemplified methods of preparation are:- making an amide from the methyl ester, with NH 3 ; esterifying the acid with CH 2 N 2 ; hydrolysing methyl esters; salt formation; separation of stereoisomers; and perfusion through mamalian liver, of an (unsubstituted-cyclohexyl) analogue. Intermediates otherwise prepared are the ethyleneketals and a semicarbazone of cyclohexanones (A); the following ketones and their ethyleneketals:-4-(oxocyclohexyl)benzyl chlorides and cyanides, 4-(oxocyclohexyl)phenylsuccinic acids; 4-(oxocyclohexyl)phenylsuccinic anhydrides; the alpha-cyano derivatives of 4- (oxocyclohexyl)phenylacetic and -succinic acids, ethyl esters, ethyleneketals; methyl 5-(4- oxocyclohexyl)indane- 1 - carboxylate, ethyleneketal; and 5-(oxocyclohexyl)-3-oxoindane- 1-carboxylic acids. Therapeutic compositions for oral, parenteral or rectal administration comprise the above acids, esters, salts and amides, which have antiinflammatory, analgesic, antipyretic and antirheumatic activity.