BigPatents India

An improved for the preparation of indole derivatives is provided comprising (a) reacting a Wittig reagent of the general formula II, wherein R is independently a straight or branched C1-C12 alkyl group, a substituted or unsubstituted aryl or an arylalkyl; R1 is a straight or branched C1-C12 alkyl group, a substituted or unsubstituted C3-C6 cycloalkyl group or a substituted or unsubstituted phenyl group; R2 is a substituted or unsubstitued hydrocarbon group of 1 to about 12 carbon atoms; R3 and R4 independently are hydrogen, C1-C6 straight or branched alkyl group, C1-C6 alkoxy; each R5 are the same or different and are hydrolysable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolysable cyclic protecting group, or each R5 is bonded to the same substituent which is bonded to each oxygen atom to form a hydrolysable protecting group; and R6 is hydrogen, a hydrocarbon group of 1 to about 12 carbon atoms or a cation of forming a non-toxic pharmaceutically acceptable salt and X is a halogen or a hydrogen sulfate; with an aldehyde or enantiomer thereof of the general formula III wherein R5 and R6 have the aforestated meanings, in the presence of a base DQGLQVROYHQWKDYLQJDGLHOHFWULFFRQVWDQW0PHDVXUHGDWÛ&JUHDWHUWKDQDERXWDQGEK\GURO\]LQJWKH:LWWLJreaction product of step (a). Drawing: NIL Total Pages: 28 Fig. Nil