Abstract: A process for synthesis of a compound of Formula (X) wherein: R1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl, wherein each substituent group of R1 is optionally independently substituted with one to three substituents selected from C1-C3 alkyl, C1-C3 alkoxy, phenyl, and alkoxyphenyl; and R2 and R3 are each independently C1-C5 alkyl.

Abstract: A process for stereoselective synthesis of a compound of Formula (X) wherein: R1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl, wherein each substituent group of R1 is optionally independently substituted with one to three substituents selected from C1-C3 alkyl, C1-C3 alkoxy, phenyl, and alkoxyphenyl; R2 and R3 are each independently C1-C5 alkyl; R4 is C1-C5 alkyl optionally independently substituted with one to three substituent groups, wherein each substituent group of R4 is independently C1-C3 alkyl, hydroxy, halogen, amino, or oxo; and R5 is a heteroaryl group substituted with one to three substituent groups, wherein each substituent group of R5 is independently C1-C5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, alkylsulfonylamino, aminosulfonyl, C1-C5 alkylaminosulfonyl, C1-C5 dialky

Abstract: A process for stereoselective synthesis of a compound of Formula (X) or Formula (X?) wherein: R1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, C1-C5 alkoxy, C1-C5 alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, C1-C5 alkoxycarbonylamino, aminosulfonyl, C1-C5 alkylaminosulfonyl, C1-C5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, nitro, or C1-C5 alkylthio wherein the sulfur atom is oxidized to sulfoxide or sulfone, and R2 and R3 are each independently hydrogen or C1-C5 alkyl.

Abstract: A process for synthesis of a compound of Formula (X) wherein: R1 is an aryl group substituted with one to three substituent groups, wherein each substituent group of R1 is independently C1-C5 alkyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, halogen, carboxy, cyano, or trifluoromethyl, wherein each substituent group of R1 is optionally independently substituted with one to three substituents selected from C1-C3 alkyl, C1-C3 alkoxy, phenyl, and alkoxyphenyl; and R2 and R3 are each independently C1-C5 alkyl.

Abstract: A process for stereoselective synthesis of a compound of Formula (I) wherein R1, R2, R3, R4, and R5 are as described herein.

Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.

Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.