LEADER 00000nam 2200313 4500
001 AAI3117968
005 20051017073436.5
008 051017s2004 eng d
020 049665392X
035 (UnM)AAI3117968
040 UnM|cUnM
100 1 Aloise, Allen Dennis
245 10 I. Synthesis of cyclooctenones using intramolecular
hydroacylation. II. Development of a catalytic
enantioselective thiol ester aldol reaction
300 183 p
500 Source: Dissertation Abstracts International, Volume: 65-
01, Section: B, page: 0219
500 Adviser: Matthew D. Shair
502 Thesis (Ph.D.)--Harvard University, 2004
520 The discovery and development of a catalytic reaction to
synthesize cyclooctenones via intramolecular
hydroacylation is described in this thesis. Rhodium
catalysts were found to promote an intramolecular
hydrometallation of 5-cyclopropyl-pent-4-enals, followed
by cyclopropane ring fragmentation and reductive
elimination, to afford cyclooctenones. Cationic Rh(I)
catalysts, of the type [Rh(dppe)]X, were found to be
superior to neutral Rh(I) catalysts for promoting the
reaction and facilitating cyclopropane ring fragmentation.
Substituted cyclooctenones, including fused 5-8 and 6-8
ring systems, were constructed. A deuterium labeling study
indicated that E- and Z-5-cyclopropyl-pent-4-enals proceed
through different reaction mechanisms to their 8-membered
ring products
520 Also described in this thesis is the development of a
catalytic enantioselective thiol ester aldol reaction.
Methyl malonic acid half thiol esters (MAHTs) and a
variety of aldehydes were found to participate in a
decarboxylative propionate aldol reaction that directly
afforded alpha-methyl-beta-hydroxythiol esters with syn
diastereoselectivity. The reaction was catalyzed by 20
mol% of copper(II) 2-ethylhexanoate in combination with 20
mol% of 5-methoxybenzimidazole and carried out at room
temperature. The use of chiral bis(oxazoline) ligands in
combination with copper(II) triflate was found to promote
catalytic enantioselective decarboxylative aldol reactions
in up to 95% yield and 95% enantiomeric excess. A
stereochemical model is presented that accounts for the
observed aldol product distribution and stereochemistry
590 School code: 0084
590 DDC
650 4 Chemistry, Organic
690 0490
710 20 Harvard University
773 0 |tDissertation Abstracts International|g65-01B
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