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1. WO2000034252 - PROCESS FOR THE PREPARATION OF CRYPTOPHYCIN DERIVATIVES

Publication Number WO/2000/034252
Publication Date 15.06.2000
International Application No. PCT/US1999/028496
International Filing Date 02.12.1999
Chapter 2 Demand Filed 12.06.2000
IPC
C07D 273/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
273Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/-C07D271/183
C07D 413/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
CPC
C07D 273/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
273Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
C07D 413/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
413Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • ELI LILLY AND COMPANY [US]/[US]
  • UNIVERSITY OF HAWAII [US]/[US]
  • WAYNE STATE UNIVERSITY [US]/[US]
Inventors
  • DHOKTE, Ulhas, Prabhakar
  • KHAU, Vien, Van
  • MARTINELLI, Michael, John
Agents
  • ENGELMANN, John, E.
  • CROWTHER, Terence, R.
Priority Data
60/111,24407.12.1998US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF CRYPTOPHYCIN DERIVATIVES
(FR) PROCEDE DE CROTYLBORATION PERMETTANT DE PRODUIRE DES COMPOSES DE CRYPTOPHYCINE
Abstract
(EN)
Processes for the preparation of Cryptophycins of the formula (II), wherein G is (C1-C12) alkyl, (C2-C12) alkenyl, (C2-C12) alkynyl, or Ar; R1 is halogen and R2 is OH or glycinate ester; or R1 or R2 may be taken together to form an epoxide ring; or R1 or R2 may be taken together to form a bond; R3 is (C1-C6) alkyl; R7 and R8 are each independently hydrogen or (C1-C6) alkyl; or R7 and R8, may be taken together to form a cyclopropyl or cyclobutyl ring; R9 is hydrogen, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, -(CH2)m-(C3-C5)cycloalkyl or benzyl; R10, R14 is hydrogen or (C1-C6) alkyl; R11 is hydrogen, (C1-C6) alkyl, phenyl or benzyl; R50 is hydrogen or (=0); Y is CH, O, NR12, S, SO, SO2, wherein R12 is hydrogen or (C1-C3) alkyl; R6 is (C1-C6) alkyl, substituted (C1-C6)alkyl, (C3-C8)cycloalkyl, substituted (C3-C8)cycloalkyl, a heteroaromatic or substituted heteroaromatic group or a group of formula (IA), (IB) OR (IC). The processes involve an asymmetric crotylboration and, in the preferred embodiment, a subsequent asymmetric allylboration, providing for an efficient method for preparing Fragment A of the Cryptophycin molecule.
(FR)
L'invention concerne des procédés permettant de préparer des dérivés de cryptophycine. Ces procédés consistent en une crotylboration asymétrique et, dans le mode de réalisation préféré, en une allylboration asymétrique consécutive, ce qui permet d'obtenir une méthode efficace de préparation du fragment A de la molécule de cryptophycine.
Also published as
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