Patent ID: 6410731
Filing Date: 2002-06-25
Classification: A61P,C07D,C07F

Abstract:
A method of synthesizing a compound having the formula via a cascade radical 4+1 annulation wherein the precursor or the precursor is reacted with an arylisonitrile having the formula wherein X is a radical precursor;wherein R1 and R2 are independently the same or different and are hydrogen, â€”C(O)Rf wherein Rf is an alkyl group, an alkoxy group, an amino group or a hydroxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an aryloxy group, an acyloxy group, â€”OC(O)ORd, wherein Rd is an alkyl group, â€”OC(O)NaRb wherein Ra and Rb are independently the same or different, H, â€”C(O)Rf, an alkyl group or an aryl group, a halogen, a hydroxy group, a nitro group, a cyano group, an azido group, a formyl group, a hydrazino group, an amino group, â€”SRc, wherein Rc is hydrogen, â€”C(O)Rf, an alkyl group or an aryl group; or R1 and R2 together form a chain of three or four members selected from the group of CH, CH2, O, S, NH, or NR15, wherein R15 is an C1-C6 alkyl group; R3 is H, a halogen atom, a nitro group, an amino group, a hydroxy group, or a cyano group; or R2 and R3 together form a chain of three or four members selected from the group of CH, CH2, O, S, NH, or NR15; R4 is H, F, an amino group, a C1-3 alkyl group, a C2-3 alkenyl group, a C2-3 alkynyl group, a trialkylsilyl group or a C1-3 alkoxy group; R5 is a C1-10 alkyl group, an alkenyl group, an alkynyl group, or a benzyl group; R13 is H, F or â€”CH3; and R6 is H, an alkyl group, â€”Si(R8R9R10) or â€”(R7)Si(R8R9R10), wherein R7 is an alkylene group, an alkenylene group, or an alkynylene group; and R8, R9 and R10 are independently a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group, an aryl group or a â€”(CH2)NR11 group, wherein N is an integer within the range of 1 through 10 and R11 is a hydroxy group, an alkoxy group, an amino group, an alkylamino group, a dialkylamino group, a halogen atom, a cyano group, â€”SRc or a nitro group.