Abstract: A synthetic process for producing bortezomib comprising converting racemic boronic esters, such as the pinacol ?-aminoboronic ester, into mixtures of diastereomers [6] by reaction with a suitably protected L-phenylalanine derivative (see Scheme 3), such as N—BOC-L-phenylalanine. The protecting group of the L-phenylalanine moiety is then removed, such as by reacting the diastereomers [6] with an acid, such as hydrochloric acid, to form a mixture of amine salt diastereomers [7] which is then subjected to conditions under which the desired diastereomer (R,S)-[7] is selectively isolated, such as by crystallization, chromatography or stereoselective hydrolysis. The separated desired diastereomer (R,S)-[7] is then converted into bortezomib or bortezomib anhydride.

Abstract: The present invention provides for synthetic processes for the making of substituted 3-((pyrrol-2-yl)methylene)-2-pyrrolones, including sunitinib. The present invention also provides for a process of crystallizing substantially pure sunitinib L-malate.

Abstract: A process of making entecavir comprising converting a compound of formula (M5) to entecavir, wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.

Abstract: The present invention provides efficient and economical methods for synthesis of (?)-2-exo-morpholinoisoborne-10-thiol, its enantiomer, and related chiral catalysts. Novel compounds and methods of asymmetric synthesis are also disclosed.

Abstract: A process of making Form A of atazanavir sulfate comprises: a) mixing atazanavir free base with a solvent selected from the group consisting of methanol (MeOH), ethanol (EtOH), isopropanol (IPA), N-methylprrolidone (NMP) and combinations thereof; b) reacting sulfuric acid with the atazanavir free base in the mixture formed in step a) to form a reaction solution comprising atazanavir sulfate; c) mixing an antisolvent with the reaction solution; d) seeding the mixture formed in step c) with an effective amount of Form A of atazanavir sulfate to form a seeded mixture comprising Form A of atazanavir sulfate; and e) isolating Form A of atazanavir sulfate in solid form from the seeded mixture; wherein the antisolvent is selected from the group consisting of methyl tert-butyl ether (MTBE), ethyl acetate (EtOAc), acetonitrile (MeCN), isopropyl acetate (IPAc), cyclohexane, and combinations thereof. In one alternative, step c) may be performed before step b).

Abstract: The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.

Abstract: The present application provides intermediates for preparing prostaglandin analogues and processes for preparing prostaglandin analogues and intermediates thereof. The intermediates include: A compound of formula (6): R1 represents H, C1-C5-alkyl, or benzyl, in particular isopropyl.

Abstract: The present invention provides for new crystalline and amorphous forms of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione, and methods of making the same.

Abstract: The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p.

Abstract: The present invention provides a process for making lapatinib and its pharmaceutically acceptable salt by use of new intermediates. A new process for obtaining a pharmaceutical form of lapatinib ditosylate monohydrate is also provided.

Abstract: A method of purifying a compound from a mixture through a chromatographic column loaded with a column adsorbent. The method comprises: applying the mixture to the chromatographic column; eluting the mixture with an elution solvent composition; and collecting the compound; wherein at least one of the column adsorbent and elution solvent is selected based on one of solubility parameters of the compound, column adsorbent, elution solvent, and conformation energy of the compound.

Abstract: A process for the preparation of cladribine of API grade is provided by direct coupling of O-protected 2-deoxy-ribofuranose with silylated 2-chloroadenine followed by deprotection of the resultant protected nucleoside in a separate step and then a purification step. Following the coupling, the desired N-9-glycosylated ?-anomer of the nucleoside is directly isolated as a solid from the coupling reaction mixture by filtration in relatively high purity and yield, and it does not require purification.

Abstract: A process of making a polylpeptide or a pharmaceutically acceptable salt thereof comprises reacting a L-lysine protected polypeptide, which comprises L-alanine, L-tyrosine, L-glutamate, and L-lysine that is protected with a protecting group, with a tetraalkylammonium hydroxide in water to remove the protecting group.

Abstract: A process of synthesizing a 5-azacytosine nucleoside, such as azacitidine and decitabine, comprises coupling a silylated 5-azacytosine with a protected D-ribofuranose of formula in the presence of a sulfonic acid catalyst.

Abstract: Crystalline granisetron hydrochloride characterized by a powder x-ray diffraction pattern with peaks at about 14.3, 20.4, and 23.0±0.2 degrees two-theta and process of making the same are disclosed.

Abstract: Provided are systems, apparatus, materials and methods for directly monitoring products and intermediates of solid phase chemical synthesis such as solid phase peptide synthesis.

Abstract: A crystalline polymorph of 7-ethyl-10-hydroxycamptothecin exhibiting an X-ray diffraction pattern having peaks at 10.9±0.2, 13.2±0.2, 23.9±0.2, and 26.1±0.2 2-theta degree.

Abstract: The present application discloses derivatives of 8-epiblechnic acid and use thereof in treating a disease related to endothelin receptor A or endothelin-1 (ET-1) over-expression, such as hypertension, cancer, atherosclerosis, and myocardial infarction.

Abstract: The present invention provides for an efficient process for making pramlinitide, as well as novel intermediates for the making of the same.

Abstract: The present invention provides a system and method for real-time continuously monitoring of oligonucleotide synthesis in solution phase.