Fujirebio Inc.

Hisako Kobayashi

Hiroshi Ikawa

Masakatsu Matsumoto

Nobuko Watanabe

Eiko Mori

Tetsuaki Yamaura

Misao Aoyama

Miwa Ishihara

A compound having the structure: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are each independently a hydrogen atom, an alkyl group or an aryl group, or wherein R.sup.2 and R.sup.3 together and R.sup.4 and R.sup.5 together are joined as a cycloalkyl group; wherein R.sup.6 is a hydroxyl group, an alkoxyl group, an aralkyloxy group, or --OSi (R.sup.8 R.sup.9 R.sup.10) in which R.sup.8, R.sup.9 and R.sup.10 are each independently an alkyl group or a phosphate salt group and R.sup.7 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxyl group.

1,2-dioxetane derivatives

A 1,2-dioxetane derivative of formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are each independently a hydrogen atom, an alkyl group, or an aryl group, R.sup.2 and R.sup.3 together and R.sup.4 and R.sup.5 together can be joined as a cyclo-alkyl group, R.sup.6 is a hydroxyl group, an alkoxyl group, an aralkyloxy group, --OSi(R.sup.8 R.sup.9 R.sup.10) in which R.sup.8, R.sup.9 and R.sup.10 are each independently an alkyl group, or a phosphate salt, and R.sup.7 is a hydrogen atom, a halogen atom, an alkyl group, or an alkoxyl group.

1,2- Dioxetane derivatives

Methods of producing carboxylic acid ester derivatives of formulae (I) and (II), which are useful, for instance, as intermediates for producing an anti-hypercholesterolemic agent having an inhibitory effect on HMG-CoA Reductase: ##STR1## wherein R.sup.1 and R.sup.2 are independently a protective group for hydroxyl group, or R.sup.1 and R.sup.2 integrally constitute a protective group for hydroxyl groups; R.sup.3 is an alkyl group, or an aryl group; and R.sup.4 is a substituted aryl group, a substituted heterocyclic group, a substituted vinyl group, or a substituted cycloalkenyl group; and ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are respectively the same as defined in the above formula (I), are disclosed. In addition, intermediates for use in these methods of producing the carboxylic acid ester derivatives are disclosed.

Methods of producing carboxylic acid ester derivatives and intermediates

A 4-fluorobiphenyl derivative of formula (I), which is useful as a cholesterol lowering agent or a lipid lowering agent because of its strong inhibitory effect on HMG-CoA reductase), and which is also useful as an intermediate for producing the above-mentioned cholesterol lowering agent or lipid lowering agent: ##STR1## wherein A is a .omega.-oxycarbonyldihydroxybutyl group, a tetrahydropyranyl group, a .omega.-oxycarbonyl-3-oxobutyl group, a formyl group, or a cyano group; R.sup.1 is a halogen atom, an alkyl group, or a group represented by R.sup.5 O--, wherein R.sup.5 is a hydrogen atom, or an alkyl group; R.sup.2 is a hydrogen atom, an alkyl group; R.sup.3 is a hydrogen atom, or an alkyl group; R.sup.5 and R.sup.2 may form a five-membered ring or a six-membered ring in combination with the oxygen atoms to which R.sup.5 and R.sup.2 are respectively bonded, and R.sup.5 and R.sup.3 may form a five-membered ring or a six-membered ring in combination with the oxygen atom to which R.sup.5 is bonded.

4-fluorobiphenyl derivatives

A 4-fluorobiphenyl derivative of formula (I): ##STR1## wherein A is a .omega.-oxycarbonyldihydroxybutyl group of formula (II): ##STR2## wherein R.sup.2 is a hydrogen atom, an alkyl group, an alkaline metal or an alkaline earth metal; a tetrahydropyranyl group of formula (III): ##STR3## or a .omega.-oxycarbonyl-3-oxobutyl group of formula (IV): ##STR4## wherein R.sup.3 is an alkyl group; R.sup.1 is an alkyl group. This 4-fluorobiphenyl derivative is useful as an effective component for a cholesterol or lipid lowering agent.

Growing community of inventors

Tokyo, Japan

Hisako Kobayashi