Abstract: The invention provides a process for preparing 1-methylindazole-3-carboxylic acid of formula (I): which comprises reacting a methylating agent with indazole-3-carboxylic acid of formula (VI): in the presence of an alkaline earth metal oxide or alkoxide in an appropriate solvent. Also provided is a process for producing Granisetron, using the method of the present invention for producing 1-methylindazole-3-carboxylic acid.

Abstract: The present invention provides improved processes for preparing the intermediate 7-hydroxy-3,4-dihydro-2(1H)-quinolinone (7-HQ), which may be used in preparing the drug aripiprazole. Among these processes are included three efficient processes for preparing 7-hydroxy-3,4-dihydro-2(1H)-quinolinone comprising reacting N-(3-methoxyphenyl)-3-chloropropionamide with AlCl3 using novel reaction conditions thus obtaining a substantially pure product, which may be used in the subsequent steps for obtaining aripiprazole without further purification.

Abstract: The present invention provides several improved processes for preparing aripiprazole, wherein the first step comprising reacting 7-HQ with a 1,4-disubstituted-butane in biphasic reaction mixture or in a single phase solvent to obtain a 7-(4-halobutoxy)-3,4-dihydro-(1H)-quinolinone (7-HBQ) and the second step comprising reacting the 7-HBQ and 1-(2,3-dichlorophenyl)piperazine or an acid addition salt thereof in a biphasic reaction medium containing water and a water-immiscible solvent to obtain aripiprazole. Also provided are methods of purifying the 7-HBQs and aripiprazole.

Abstract: Derivatives of 1,2-benzisoxazole-3-methanesulfonic acid, which are non-hygroscopic and non-hydrated and their use as intermediates fro the preparation of zonisamide are disclosed. Further disclosed are processes of preparing zonisamide from these 1,2-benzisoxazole-3-methanesulfonic acid derivatives, processes of preparing exemplary 1,2-benzisoxazole-3-methanesulfonic acid derivatives and crystalline forms of exemplary 2-benzisoxazole-3-methanesulfonic acid derivatives. A novel process of preparing zonisamide is also disclosed.

Abstract: Disclosed is a process of preparing 1,2-benzisoxazole-3-methanesulfonamide (zonisamide). Also disclosed is a method of dehydrating sodium 1,2-benzisoxazole-3-methanesulfonate, a compound useful in the preparation of 1,2-bisoxazole-3-methanesulfonamide (zonisamide) as well as new crystalline forms of sodium 1,2-benzisoxazole-3-methanesulfonate.

Abstract: A novel process for preparing highly pure cilostazol, effected by reacting 6-hydroxy-3,4-dihydroquinolinone and 5-(4-chlorobutyl)-1-cyclohexyl-1H-tetrazole in the presence of a hydrated inorganic base, is disclosed. Further disclosed is highly pure cilostazol, and particularly highly pure cilostazol that is substantially free of 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butoxy]-1-[4-(1-cyclohexyl-1H-tetrazol-5-yl)-butyl]-3,4-dihydro-1H-quinolin-2-one.

Abstract: The invention provides a process for preparing 1-methylindazole-3-carboxylic acid of formula (I): 1

Abstract: The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH2CONH2, wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.

Abstract: The invention provides a process for the preparation of diphenylmethylthioacetamide (I) as described in Scheme 4 comprising reacting of the isothiouronium salt or its corresponding base of the formula IV with an acetamide of the formula XCH2CONH2, wherein X represents a halogen, M represents an alkali metal and A represents an anion, in a protic medium at a temperature of less than 100° C.