Ube Industries, Inc.

Nippon Chemiphar Co., Ltd.

Hiroshi Sasaki

Katsumasa Harada

Akio Matsushita

Yasuhiro Kawachi

Shigeyoshi Nishino

Kunio Kobayashi

Masao Yamamoto

Preparation of 2-(10,11-dihydro-10-oxodibenzo-[b,f]thiepin-2-yl)

Methyl (3R, 6E)-3-�(tert-butyldimethylsilyl)oxy!-7-�2', 6'-diisopropyl-4'-(4'-fluorophenyl)-5'-(methoxymethyl)pyridin-3'-yl!-5-oxy -6-heptenoate or other 3-oxy-5-oxo-6-heptenoic acid derivative is prepared by the reaction of an aromatic aldehyde and an oxyglutaric acid derivative in an aliphatic alcohol containing a small amount of water in the presence of an alkali metal carbonate or hydrogen carbonate.

Preparation of 3-oxy-5-oxo-6-heptenoic acid derivatives

A process for preparing an oxyglutaric acid ester derivative of the formula: ##STR1## in which each of R.sup.1 and R.sup.2 is C.sub.1-5 alkoxy, C.sub.1-7 aralkyloxy, C.sub.7-9 halogenated aralkyloxy or phenyl, R.sup.4 is a hydroxyl-protecting group, and R.sup.5 is C.sub.1-10 alkyl which may have a substituent, comprises the steps of reacting a methyl phosphonate derivative or methyl phosphine oxide derivative with an oxyglutaric acid mono-ester to give a reaction product which comprises an oxyglutaric acid derivative having a phosphorus-containing group and a pentenedioic acid mono-ester (by-product), removing the pendenedioic acid mono-ester from the reaction product to isolate the oxyglutaric acid derivative, and converting the isolated oxyglutaric acid derivative into the oxyglutaric acid ester derivative. A process for obtaining an optically active oxyglutaric acid ester derivative is also disclosed.

Process for preparation of oxyglutaric acid ester derivatives

Methyl (3R,6E)-3-�(tert-butyldimethylsilyl)oxy!-7-�2',6'-diisopropyl-4'-(4'-fluor ophenyl)-5'-(methoxymethyl)pyridin-3'-yl!-5-oxy-6-heptenoate or other 3-oxy-5-oxo-6-heptenoic acid derivative is prepared by the reaction of an aromatic aldehyde and an oxyglutaric acid derivative in an aliphatic alcohol containing a small amount of water in the presence of an alkali metal carbonate or hydrogen carbonate.

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Yamaguchi, Japan

Hiroshi Sasaki