(19)

(11)

EP 0 543 969 A1

(12)

(43) Date of publication: 02.06.1993 Bulletin 1993/22 (21) Application number: 92912059.0 (22) Date of filing: 08.05.1992

(51) International Patent Classification (IPC):  C07D 317/ 20( . ) C07C 29/ 04( . ) C07C 31/ 20( . ) C07C 67/ 31( . ) C07C 69/ 732( . ) C07D 453/ 04( . ) C07B 61/ 00( . ) C07C 29/ 48( . ) C07C 33/ 26( . ) C07C 69/ 675( . ) C07D 317/ 30( . ) (86) International application number: PCT/US1992/003940 (87) International publication number: WO 1992/020677 (26.11.1992 Gazette 1992/29)

(84) Designated Contracting States: AT BE CH DE DK ES FR GB GR IT LI LU MC NL SE (30) Priority: 13.05.1991 US 19910699183 (71) Applicant: MASSACHUSETTS INSTITUTE OF TECHNOLOGY Cambridge, Massachusetts 02139 (US)

(72) Inventors: SHARPLESS, K., Barry LaJolla, CA 92121 (US) BELLER, Matthias D-3501 Eder Munde (DE) BLACKBURN, Brent San Francisco, CA 94124 (US) KAWANAMI, Yasahiro Brookline, MA 02146 (US) KWONG, Hoi-Lun Somerville, MA 02143 (US) OGINO, Yasukazu Brookline, MA 02146 (US) SHIBATA, Toinoyuki Arakawa-ku, Tokyo 116 (JP) UKITA, Tatsuzo Hyogo 663 (JP) WANG, Lisa Boston, MA 02116 (US) (74) Representative: Holdcroft, James Gerald, Dr., et al  Graham Watt & Co., Riverhead Sevenoaks, Kent TN13 2BN Sevenoaks, Kent TN13 2BN (GB)