Intermediates for the production of epipodophyllotoxin and related compounds and processes for the preparation and use thereof

• Main Authors: VYAS; DOLATRAI M, SKONEZNY; PAUL M
• Format: Patent
• Language: English
• Published: 09.06.1992
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the and present invention wherein R1 and R2 each are independently hydrogen or (lower)alkoxy, or R1 ll and R2, taken together, is methylenedioxy; R4 and R6 each are independently hydrogen or (lower)alkoxy; and R5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present ivnention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.