Abstract: Disclosed is a process for preparing a treprostinil salt. The process involves the step of dissolving treprostinil in a water-miscible organic solvent to form a treprostinil solution. The treprostinil solution is reacted with an aqueous basic solution containing an alkali metal cation to form treprostinil salt. Allowing crystallization of the treprostinil salt to take place, and then collecting the treprostinil salt formed.

Abstract: A para-methoxy protected benzaldehyde useful in preparation of treprostinil, and of formula: (Formula (1)) is prepared by subjecting to Claisen re-arrangement a substituted benzaldehyde of formula (1a): (Formula (Ia)) to form the m-hydroxy-substituted benzaldehyde of formula (1b): (Formula (Ib)) and then reacting compound (1b) with a p-methoxybenzyl (PMB) compound to form a PMB-substituted benzaldehyde of formula (1).

Abstract: Disclosed is a process for preparing a treprostinil salt. The process involves the step of dissolving treprostinil in a water-miscible organic solvent to form a treprostinil solution. The treprostinil solution is reacted with an aqueous basic solution containing an alkali metal cation to form treprostinil salt. Allowing crystallization of the treprostinil salt to take place, and then collecting the treprostinil salt formed.

Abstract: A para-methoxy protected benzaldehyde useful in preparation of treprostinil, and of formula: (Formula (1)) is prepared by subjecting to Claisen re-arrangement a substituted benzaldehyde of formula (1a): (Formula (Ia)) to form the m-hydroxy-substituted benzaldehyde of formula (1b): (Formula (Ib)) and then reacting compound (1b) with a p-methoxybenzyl (PMB) compound to form a PMB-substituted benzaldehyde of formula (1).

Abstract: An industrially acceptable process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine from a cis/trans mixture of isomers. Treatment of the mixture with an organic sulfonic acid generates a less soluble acid addition salt that is enriched in the cis-isomer. Recrystallization or pulping using various organic solvents allows for enrichment of the cis-isomer by filtration. These new sulfonic acid salts of the cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine prepared according to the present invention could be further converted into the hydrochloride salt by any known procedures such as treatment with a base and then hydrochloric acid salt formation or exchange of the sulfonic acid salt with hydrochloric acid.

Abstract: An industrially acceptable process for the preparation of 2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine. The cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine is known generally as Cevimeline.

Abstract: A process for the preparation and purification of Eplerenone is described wherein hydroxylated impurities are removed using a novel derivatization procedure.

Abstract: An industrially acceptable process for the preparation and purification of cis-2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine from a cisitrans mixture of isomers. Treatment of the mixture with an organic sulfonice acid generates a less soluble acid addition salt that is enriched in the cis-isomer. Recrystallization or pulping using various organic solvents allows for enrichment of the cis-isomer by filtration. These new sulfonic acid salts of the cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine prepared according to the present invention could be further converted into the hydrochloride salt by any known procedures such as treatment with a base and then hydrochloric acid salt formation or exchange of the sulfonic acid salt with hydrochloric acid.

Abstract: An industrially acceptable process for the preparation of 2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine. The cis-isomer of 2-methylspiro(1,3-oxathiolane-5,3?)quiniclidine is known generally as Cevimeline.

Abstract: A process for the preparation and purification of Eplerenone is described wherein hydroxylated impurities are removed using a novel derivatization procedure.

Abstract: The present invention provides for a novel process for the preparation of Midodrine or a pharmaceutically acceptable salt thereof comprising: (a) a step of reacting 2-amino-1-(2?,5?-dimethoxyphenyl) ethanol of formula (I) with an N-protected glycine of formula (II) containing an amino protecting group in the presence of 1,1?-carbonyldiimidazole (CDI); and (b) removing the amino protecting group by deprotection formula (I), formula (II), wherein R1 is a benzyl, triphenylmethyl, tert-butyloxycarbonyl, or a benzyloxycarbonyl group. This results in an unexpectedly efficient and cost-effective process. Additionally, the process is simple and safe as all the intermediates and reagents involved in the process pose no safety risks. Further reaction of Midodrine with a pharmaceutically acceptable acid affords a pharmaceutically acceptable salt thereof. Preferably, the pharmaceutically acceptable salt obtained from the process according to the present invention is Midodrine Hydrochloride.

Abstract: A process for the preparation of a polypeptide designated in the present invention as 1, composed of the following amino acid units in the structure, namely: L-alanine, L-glutamic acid, L-lysine and L-tyrosine randomly arranged in the polypeptide 1, or pharmaceutically acceptable salts thereof, comprising the steps of: (a) polymerization of a mixture of the N-carboxyanhydrides of L-alanine, L-tyrosine, a protected L-glutamate and a protected L-lysine to obtain protected copolymer 6 or salt thereof; (b) deprotection of the protected copolymer 6 (or salt thereof) to produce polypeptide 1 or a pharmaceutically acceptable salt thereof in one single step; (c) separation and purification of the polypeptide 1 (or a pharmaceutically acceptable salt) to obtain a purified polypeptide 1

Abstract: A process for the resolution of each of the enantiomers of methyl-?-5-[4,5,6,7-tetrahydro[3,2-c]thienopyridyl]-(2-chlorophenyl)acetate and salts thereof by diastereomeric crystallization comprising the use of a single optically active resolving agent and at least one solvent.

Abstract: A process for the preparation of a polypeptide designated in the present invention as 1, composed of the following amino acid units in the structure, namely: L-alanine, L-glutamic acid, L-lysine and L-tyrosine randomly arranged in the polypeptide 1, or pharmaceutically acceptable salts thereof, comprising the steps of: