Abstract: The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine.

Abstract: The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-1{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine.

Abstract: Polymorphic, amorphous and hydrated forms of the title compound having the following structure: are disclosed. The compound is a potent and selective cyclooxygenase-2 (COX-2)inhibitor.

Abstract: The present invention provides an efficient process for the preparation of benzothiophenecarboxamide PGD2 antagonist, S-5751.

Abstract: The present invention provides an efficient process for the preparation of benzothiophenecarboxamide PGD2 antagonist, S-5751.

Abstract: This invention is concerned with a novel polymorphic forms of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethyl-amino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic forms have advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethylamino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Abstract: A process of synthesizing a compound of the formula 1: is disclosed, which comprises reacting a compound of the formula 2: with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.

Abstract: The present invention is directed to the compound 4-N,N-dimethylaminomethyl-5-formyl-1,2,3-triazole which is a valuable intermediate in the preparation of phamaceutical compounds. The present invention is further directed to a novel convergent process for the preparation of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)-ethoxy)-4-(5-(dimethylamino) methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)-morpholine which is a potent and selective substance P (or neurokinin-1) receptor antagonist useful as a therapeutic agent.

Abstract: The present invention is concerned with a novel linear process for the preparation of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl) phenyl)-ethoxy)-4-(5-(dimethylamino)methyl-1,2,3-triazol-4-yl)methyl-3-(S) -(4-fluorophenyl)-morpholine which is a potent and selective substance P (or neurokinin-1) receptor antagonist usefull as a therapeutic agent.

Abstract: The present invention is directed to a process for the preparation of the reagent dimethyl titanocene (Cp.sub.2 Ti(CH.sub.3).sub.2) from titanocene dichloride (Cp.sub.2 TiCl.sub.2) and a methyl magnesium halide, in particular, methyl magnesium chloride (CH.sub.3 MgCl). The instant process provides the desired reagent in a manner which is generally less hazardous and more economical than previous methods.

Abstract: The present invention is directed to a process of making spirocycles of general structural formula: ##STR1## where R.sub.1 is selected from the group consisting of CO--C.sub.1-3 alkyl, cyano, carboxy, carboxy C.sub.1-6 alkyl ester, carboxamide, C.sub.1-6 alkyl sulfinyl, C.sub.1-6 alkyl sulfonyl, C.sub.1-6 methanesulfonamide and halogen; R.sub.2 is selected from the group consisting of keto or alcohol, R.sub.3 is cyano, resulting in compounds which are Class III antiarrhythmic.

Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is disclosed, which comprises reacting a compound of the formula 2: ##STR2## with diphenylphosphine in the presence of an amine base and a nickel catalyst to produce a compound of formula 1.