Abstract: Provided herein are processes for synthesizing compounds useful as EGFR modulators.

Abstract: This invention provides a novel method for the preparation of 2,3-disubstituted -4-oxy-cyclopentan1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted -4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

Abstract: The present application discloses a stereoselective process for the preparation of ?-C-arylglucosides that does not require the use of conventional carbohydrate protecting groups. In one embodiment, the stereoselective process comprises the preparation of the compound of formula I: the process comprising: a) contacting 1,6-anhydro-?-D-glucopyranose with a compound of formula II, R1R2R3Al, in a solvent to form a first reaction mixture; b) contacting the first reaction mixture of step a) with a second reaction mixture to form a third reaction mixture, wherein the second reaction mixture is prepared by contacting an organoaluminum compound of formula III, R4aR5bAlXc, with a compound of formula IV, ArM; and c) contacting the third reaction mixture with a reagent to form the compound of the formula I.

Abstract: This invention provides a novel method for the preparation of 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted-4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

Abstract: The present application discloses a stereoselective process for the preparation of ?-C-arylglucosides that does not require the use of conventional carbohydrate protecting groups.

Abstract: Intermediates of the following formulae for the preparation of lubiprostone:

Abstract: The present invention provides amorphous forms and the crystalline complexes of SGLT2 inhibitors as a novel material, in particular in pharmaceutically acceptable form. The crystalline forms of SGLT2 inhibitor canagliflozin are designated as Forms CS1, CS2, CS3, CS4 and CS5.

Abstract: The present invention provides processes (e.g., arylation reaction) for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors.

Abstract: Intermediates of the following formulae for the preparation of lubiprostone:

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: Processes for preparing and purifying lubiprostone are disclosed. Intermediates and preparation thereof are also disclosed.

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 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 invention provides processes for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors.

Abstract: A compound of formula (X): which can be used as an intermediate to make lapatinib or its pharmaceutically acceptable salt.

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: A process for making clofarabine comprising: fluorinating a compound of formula VII wherein each R4 is independently a hydroxy protecting group, OR6 is a leaving group, with a fluorinating agent in the presence of guanidine carbonate to give a compound of formula VIII: wherein R4 is as defined above; and deprotecting the compound of formula VIII to give the clofarabine.

Abstract: A compound of formula (X): which can be used as an intermediate to make lapatinib or its pharmaceutically acceptable salt.

Abstract: A method for producing a ?-enriched protected decitabine comprising: a) coupling a protected 2-deoxy-ribofuranose with a protected 5-azacytosine in the presence of a catalyst to form a reaction mixture comprising the protected decitabine of formula I; and b) quenching the reaction mixture of step a) with a base. The ?-enriched protected decitabine so made may be deprotected to produce a decitabine product in a high yield and purity.

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.