Patent classifications
C07C51/08
PROCESSES FOR PREPARING ACC INHIBITORS AND SOLID FORMS THEREOF
The present disclosure provides solid forms, including a salt or co-crystal, of Compound I:
##STR00001##
which exhibits Acetyl-CoA carboxylase (ACC) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.
PROCESSES FOR PREPARING ACC INHIBITORS AND SOLID FORMS THEREOF
The present disclosure provides solid forms, including a salt or co-crystal, of Compound I:
##STR00001##
which exhibits Acetyl-CoA carboxylase (ACC) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.
Process for the preparation of 9 beta,10 alpha-progesterone (retroprogesterone)
The present invention refers to a new process for the synthesis of (9,10)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below. ##STR00001##
Process for the preparation of 9 beta,10 alpha-progesterone (retroprogesterone)
The present invention refers to a new process for the synthesis of (9,10)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below. ##STR00001##
Process for preparation of prostacyclin derivatives
The invention relates to improved method of synthesis for Treprostinil comprising condensation reaction of the carbonyl compound having allyl, alkyl, crotyl or MEM-protected phenolic hydroxyl group, compound (4) with a hydroxyl-protected alkynol (5) to give the condensation product, compound (6). Subjecting compound (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gave the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents was governed by protecting groups, gave the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yielded the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts, having desired purity.
Process for preparation of prostacyclin derivatives
The invention relates to improved method of synthesis for Treprostinil comprising condensation reaction of the carbonyl compound having allyl, alkyl, crotyl or MEM-protected phenolic hydroxyl group, compound (4) with a hydroxyl-protected alkynol (5) to give the condensation product, compound (6). Subjecting compound (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gave the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents was governed by protecting groups, gave the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yielded the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts, having desired purity.
Process for preparation of prostacyclin derivatives
The invention relates to improved method of synthesis for Treprostinil comprising condensation reaction of the carbonyl compound having allyl, alkyl, crotyl or MEM-protected phenolic hydroxyl group, compound (4) with a hydroxyl-protected alkynol (5) to give the condensation product, compound (6). Subjecting compound (6) to oxidation, reduction, hydroxyl protection and carbonylation, cyclization reactions gave the tricyclic derivative (10). Further reactions comprising reduction, hydrogenation and deprotection of the phenolic and side-chain hydroxyl groups, wherein the sequence and choice of reagents was governed by protecting groups, gave the triol intermediate, compound (14). Cyanoalkylation at phenolic hydroxyl functionality and further hydrolysis yielded the prostacyclin compound, Treprostinil (1) and its pharmaceutically acceptable salts, having desired purity.
PROCESS FOR THE PREPARATION OF 9 BETA,10 ALPHA-PROGESTERONE (RETROPROGESTERONE)
The present invention refers to a new process for the synthesis of (9,10)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below.
##STR00001##
PROCESS FOR THE PREPARATION OF 9 BETA,10 ALPHA-PROGESTERONE (RETROPROGESTERONE)
The present invention refers to a new process for the synthesis of (9,10)-pregn-4-ene-3,20-dione, commonly known as retroprogesterone, having the formula (1) shown below.
##STR00001##
Process to prepare treprostinil, the active ingredient in Remodulin®
This present invention relates to an improved process to prepare prostacyclin derivatives. One embodiment provides for an improved process to convert benzindene triol to treprostinil via salts of treprostinil and to purify treprostinil.