Abstract: Disclosed herein are processes for the preparation of fused heteroaryl dihydro pyrimidine compounds, or salts or stereoisomers thereof, which are useful for the treatment and prophylaxis of hepatitis B virus infections using compounds of formula IX or stereoisomers thereof, wherein a disclosed process comprises a. reacting a compound formula II with hydrogen in the presence of a solvent and a palladium catalyst or a platinum catalyst, to form a compound of formula III: b. reacting the compound of formula III, or a salt or stereoisomer thereof, with a hydrolase selected from the group consisting of an amidase and a peptidase, or a mixture thereof, to form a compound of formula I: or a salt or stereoisomer thereof, c.

Abstract: The present invention relates to a process for producing a chiral aromatic amine comprising the steps of a) providing an aromatic imine, and b) contacting the aromatic imine from step a) with an imine reductase, thereby stereoselectively reducing the aromatic imine with the imine reductase to a chiral aromatic amine and to novel imine reductases which are capable to catalyse the reaction.

Abstract: The present invention relates to a mutant ketoreductase with at least one mutation at position 241, a nucleic acid encoding the mutant ketoreductase, a vector comprising the nucleic acid, a method for the enzymatic reduction of a ketone and the formation of a chiral alcohol with the mutant ketoreductase, the use of the mutant ketoreductase for the reduction of ketones and the formation of chiral alcohols as well as the use of the method for the preparation of pharmaceutically active serine/threonine protein kinase inhibitors.

Abstract: The present invention relates to a mutant ketoreductase, a nucleic acid encoding the mutant ketoreductase, a vector comprising the nucleic acid, a method for the enzymatic reduction of a prochiral ketone and the formation of a chiral alcohol with the mutant ketoreductase, the use of the mutant ketoreductase for the preparation of chiral alcohols as well as the use of the method for the preparation of pharmaceutically active morpholine compounds.

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

Abstract: The invention relates to a novel process for the preparation of a chiral piperazine-2- carboxylic acid or of a salt thereof of the formula (I). The chiral piperazine-2-carboxylic acid derivatives of the formula (I) are key intermediates for the preparation of fused heteroaryl dihydro pyrimidines which are useful for the treatment and prophylaxis of hepatitis B virus infections.

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

Abstract: The present invention relates to the use of a protein as a hydroxylase, a host cell comprising the protein, the use of the protein or host cell in the production of hydroxy-pipecolic acid (HPA), a method of production HPA, methods of producing the protein, a mutant protein and a nucleic acid encoding the mutant protein and a vector comprising a nucleic acid encoding the protein.

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.