Claims for Patent: 5,514,826

Summary for Patent: 5,514,826

Title:	Vinyl sulfenic acid derivatives
Abstract:	The present invention is directed to novel vinyl sulfenic acid derivatives, useful for the synthesis of benzo b!thiophenes, in particular 2-arylbenzo b!thiophenes.
Inventor(s):	David W. Hoard, Wayne D. Luke
Assignee:	Eli Lilly and Co
Application Number:	US08/483,607
Patent Claims:	1. A compound of the formula ##STR16## wherein: R1 is hydrogen, C1 -C4 alkoxy, arylalkoxy, halo, or amino;R2 is hydrogen, C1 -C4 alkoxy, arylalkoxy, halo, or amino; R4 is OSi(R)3, NR5 R6, or SR8 ; each R is independently C1 -C6 alkyl, aryl, or arylalkyl; R5 and R6 are independently hydrogen, C1 -C6 alkyl, arylalkyl, or aryl; or R5 and R6 together with the nitrogen atom form a ring selected from piperidine, pyrrolidine, morpholine, or hexamethylimine; and R8 is C1 -C6 alkyl, aryl, or arylalkyl. 2. The compound of claim 1 wherein:R1 is hydrogen, C1 -C4 alkoxy, or arylalkoxy; and R2 is hydrogen, C1 -C4 alkoxy, or arylalkoxy. 3. The compound of claim 2 wherein:R4 is OSi(R)3 ; and each R is independently C1 -C6 alkyl, aryl, or arylalkyl. 4. The compound of claim 3 wherein R4 is OTMS, OTES, OTIPS, ODMIPS, ODEIPS, OTDS, OTBDMS, OTBDPS, OTBS, OTPS, ODPMS, or OTBMPS. 5. The compound of claim 4 wherein R4 is OTMS, OTES, ODMIPS, ODEIPS, OTBDMS, OTBS, or OTPS. 6. The compound of claim 5 wherein R1 and R2 are C1 -C4 alkoxy. 7. The compound of claim 6 wherein R1 and R2 are methoxy, and R4 is OTMS. 8. The compound of claim 2 wherein:R4 is NR5 R6 ; and R5 and R6 are independently hydrogen, C1 -C6 alkyl, arylalkyl, or aryl; or R5 and R6 together with the nitrogen atom form a ring selected from piperidine, pyrrolidine, morpholine, and hexamethylimine. 9. The compound of claim 8 wherein R5 and R6 are independently hydrogen, C1 -C6 alkyl, or arylalkyl; or R5 and R6 together with the nitrogen atom form a ring selected from piperidine and pyrrolidine. 10. The compound of claim 9 wherein R1 and R2 are C1 -C4 alkoxy. 11. The compound of claim 10 wherein R1 and R2 are methoxy, and R5 and R6 are methyl. 12. The compound of claim 10 wherein R1 and R2 are methoxy, R5 is hydrogen, and R6 is benzyl. 13. The compound of claim 2 wherein:R4 is SR8 ; and R8 is C1 -C6 alkyl, aryl, or arylalkyl. 14. The compound of claim 13 wherein R8 is C1 -C6 alkyl or arylalkyl. 15. The compound of claim 14 wherein R8 is C1 -C6 alkyl. 16. The compound of claim 15 wherein R1 and R2 are C1 -C4 alkoxy. 17. The compound of claim 16 wherein R1 and R2 are methoxy, and R8 is ethyl.