f)
Pergamon
PII: S0040-4020(97) 10141-7
letrahedron, Vol..53, NO..50, pp. 17201-17210, 1997
O 1997 Elsevier Science Ltd
All rights reserved. Printed in Great Britain
0040-4020/97 $17.00 + 0.00
Funetionalised Propargyllithium Reagents
Cecilia G6mez, Fernando F. Huerta, Isidro M. Pastor and Miguel Yus*
Departamento de Quimica Org,4nica, Facultad de Ciencias, Universidad de Alicante, Apdo. 99, 03080 Alicante, Spain
Abstract : The reaction of chlorinated acetylenic ether or amines I with lithium and a catalytic amount of
DTBB (5%), in the presence of different electrophiles [priCHO, ButCHO, PhCHO, Me2CO, (CH2)5CO,
Me3SiCI] in THF at -78 or -105°C leads, after hydrolysis with water, to the corresponding products 2. The
same process applied to the previously deprotonated chloroalcohol 4a or the secondary amine 4b can be
carried out in a two-step reaction giving the expected products 6 by using several electrophiles [PrJCHO,
ButCHO, PhCHO, Me2CO, (CH2)5CO, Me3SiCI] at-78°C. © 1997 Elsevier Science Ltd.
INTRODUCTION
An inherent problem concerning both nucleophilic or electrophilic propargylic substitution is that this
process can yield the expected propargylic product of the type I, together with the corresponding allenic
system of the type II, this last one being in many cases the most important.
A B
R A Nu
I II
A B
A E
+ I II
When at the other propargylic position is a heteroatom, the corresponding organometallic species are, in
general, unstable due to their tendency to suffer decomposition, even at low temperatures, to give a 8-
elimination reaction which, for instance in the case of the corresponding organolithium compound III, would
give a cumulenic compound IV.I
17201