Abstract: The invention relates to a subtilisin BPN? variant or homologue thereof, having new mutations compared to subtilisin BPN? represented by SEQ ID NO: 2 or a homologue sequence thereof. Such mutations may occur at amino acid positions L96, D99, A223 or S224. The invention further relates to a method for enzymatically synthesizing a peptide by coupling peptide fragments, wherein the coupling is catalyzed by the subtilisin BPN? variant or homologue thereof.

Abstract: The present invention relates to an improved process for the preparation of a compound of Formula (1), The invention also provides improved processes for the preparation of intermediates used in the synthesis of Formula (1). The compound of Formula (1) is used in the synthesis of Semaglutide.

Abstract: The present invention relates to the polymorphic forms of Belinostat. The invention also relates to the process for the preparation of the polymorphic forms of Belinostat. This invention further relates to pharmaceutical composition of said polymorphic forms of Belinostat and use thereof in the treatment of a patient in need thereof.

Abstract: The invention provides a method for the cleavage of Fmoc group characterized by using a solution comprising 3-(diethylamino)propylamine. In particular, it provides a method for the preparation of peptides in solid phase wherein Fmoc protected amino acids are used and the Fmoc group is cleaved by a solution comprising 3-(diethylamino)propylamine.

Abstract: The present provides a simple, convenient and time-efficient process for the preparation of propofol. Particularly, the present invention provides an improved process for the preparation of propofol using a heterocyclic base for the decarboxylation reaction. The present invention provides a time-efficient process for the preparation of propofol with high yield and purity.

Abstract: The present invention relates to an improved process for the preparation of a compound of formula (I), wherein PG1 may be independently selected from tert-butyloxycarbonyl (Boc), phthaloyl, 9-fluorenylmethyloxycarbonyl (Fmoc), triphenylmethyl (Trityl), carboxybenzyl (Cbz), trifluoroacetyl, benzyl (Bn), benzylidene, methanesulfonyl (Mesyl), toluene sulfonyl (Tosyl) or acyl; its isolation as solid and use for the preparation of the compound of formula (IV), in particular the compound of formula (IV) i.e. [(1R)-3-methyl-1[[(2S)-1-oxo-3-phenyl-2-[(pyrazinylcarbonyl) amino]propyl]amino]butyl] boronic acid with more than 99.95% chiral purity, as measured by HPLC.

Abstract: The present invention provides an improved process for the preparation of high purity glucagon comprising the use of Xmb-protected amino acids, wherein may Xmb include, e.g., 2,4,6-trimethoxybenzyl, 2,4-dimethoxybenzyl, or 2-hydroxy-4-methoxybenzyl. The process also comprises the use of building blocks such as pseudoprolines to avoid aggregation and obtain the product in high yield and purity.

Abstract: The present invention provides an improved process for the preparation of glucagon, comprising the coupling of an N-terminal tetramer fragment with a C-terminal peptide, comprising at least one pseudoproline. The process is very efficient in avoiding aggregation and obtaining the desired product in high yield and purity.

Abstract: The present invention relates to a process for preparing the Alectinib or a pharmaceutically acceptable salt thereof using lesser reaction steps and also eliminating expensive and time-consuming column chromatography. The invention also relates to novel polymorphic forms of Alectinib and Alectinib hydrochloride.

Abstract: The invention relates to a process for the preparation of ribociclib of formula V or its salts. The invention provides novel crystalline forms of ribociclib succinate and ribociclib trifluoroacetate. The present invention also relates to pharmaceutical compositions comprising a crystalline form of ribociclib succinate and at least a pharmaceutically acceptable carrier. It further relates to the use of such compositions in the treatment of cancer.

Abstract: The present invention provides a process for the manufacture of GLP-1 analogues with high yield and purity by fragment condensation on the solid phase. In particular, it describes a convergent synthesis by condensation of a C-terminal pseudoproline fragment A with a fragment B bound to a solid support, followed by deprotection and cleavage from the support and final purification to yield the desired peptide. The invention further provides intermediates useful in the manufacturing process.

Abstract: The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof.

Abstract: The invention provides a method for the cleavage of Fmoc group characterized by using a solution comprising 3-(diethylamino)propylamine. In particular, it provides a method for the preparation of peptides in solid phase wherein Fmoc protected amino acids are used and the Fmoc group is cleaved by a solution comprising 3-(diethylamino)propylamine.

Abstract: The present invention provides a manufacturing process for the preparation of degarelix by using Fmoc protected amino acids as building blocks, wherein the Fmoc group is cleaved by treatment with tert-butylamine.

Abstract: The present invention provides a process for the manufacture of GLP-1 analogues with high yield and purity by fragment condensation on the solid phase. In particular, it describes a convergent synthesis by condensation of a C-terminal pseudoproline fragment A with a fragment B bound to a solid support, followed by deprotection and cleavage from the support and final purification to yield the desired peptide. The invention further provides intermediates useful in the manufacturing process.

Abstract: The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

Abstract: The present invention relates to a process for preparing alectinib, or a pharmaceutically acceptable salt thereof, and to related intermediates.

Abstract: The present invention relates to a process for preparing the Alectinib or a pharmaceutically acceptable salt thereof using lesser reaction steps and also eliminating expensive and time-consuming column chromatography. The invention also relates to novel polymorphic forms of Alectinib and Alectinib hydrochloride.

Abstract: The present invention provides a manufacturing process for preparing a peptide, preferably a decapeptide, such as degarelix, by incorporating p-nitro-phenylalanin in the amino acid sequence preferably during stepwise solid phase synthesis, and converting these into the required amino acids Aph(Hor) and/or D-Aph(Cbm), preferably while attached to a solid phase. The invention further provides intermediates useful in the manufacturing process.

Abstract: The present invention relates to the polymorphic forms of Belinostat. The invention also relates to the process for the preparation of the polymorphic forms of Belinostat. This invention further relates to pharmaceutical composition of said polymorphic forms of Belinostat and use thereof in the treatment of a patient in need thereof.