Taisho Pharmaceutical Co., Ltd.

Nippon Zeon Company, Ltd.

Shigeo Morimoto

Takashi Adachi

Yoshiaki Watanabe

Toshifumi Asaka

Masato Kashimura

Sadafumi Omura

Katsuo Hatayama

Kaoru Sota

Yoko Misawa

Kazunori Hanada

Kiyoshi Oguma

Masaharu Tamai

Tohru Matsunaga

Yoko Takahashi

Toshiro Yamada

Kuniaki Goto

Jiro Sawada

Hiroshi Fujisawa

Kazutoshi Mizoue

Masami Goi

Kazuto Sekiuchi

Joji Sasaki

Morihiro Mitsukuchi

Jozi Nakagami

Tadashi Eguchi

Takatoshi Nagate

Masahuru Tamai

Erythromycin A derivatives represented by the general formulawherein Ris a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 of a halogen atom, an alkoxy group 1 to 4 carbon atoms, a nitro group or an alkoxycarbonyl group having 2 to 6 carbon atoms, Ris a substituted silyl group and Ris a hydrogen atom or R, are disclosed. These compounds are useful as intermediates of the anti-bacterial agents.

Erythromycin A derivatives and method for preparing same

Erythromycin a derivatives and method for preparing same

5-O-desosaminylerythronolide a derivatives

5-O-desosaminylerythronolide derivatives

5-O-desosaminylerythronolide a derivative

6-0-methylerythromycin A derivatives

2'-position modified compound of erythromycin or its derivative

A 6-O-methylerythromycin A oxime derivative represented by the formula ##STR1## wherein X is a substituted benzyl group, a substituted phenyl group, an .alpha.-methylbenzyl group, an .alpha.-methylphenethyl group, a diphenylmethyl group, a trityl group, a dibenzosuberanyl group, or a group of the formula --(CH.sub.2).sub.n --R, and Y is a hydrogen atom, a substituted phenyl group or a 2-aminothiazol-4-ylmethylcarbonyl group, and a pharmaceutically acceptable salt thereof are disclosed. These compounds have antibacterial activity against erythromycin resistant bacteria.

6-O-methylerythromycin A oxime derivatives

Erthromycin A derivatives represented by the general formula ##STR1## wherein R.sup.1 is a group of the formula R.sup.7 CH.sub.2 -- (wherein R.sup.7 is a hydrogen group or a lower alkyl group) or a group of the formula R.sup.8 O-- (wherein R.sup.8 is a lower alkyl group), R.sup.2 is R.sup.8, a cycloalkyl group, a phenyl group or an aralkyl group.), or R.sup.2 and R.sup.7 together form an alkylene group, R.sup.3 is a hydrogen atom, a lower alkyl group, a phenyl group or an aralkyl group, or R.sup.3 and R.sup.7 together form an alkylene group, or R.sup.2 and R.sup.3 together form an alkylene group, R.sup.4 is a lower alkyl group, R.sup.5 is a substituted silyl group, and R.sup.6 is a hydrogen atom or R.sup.5, are disclosed. These compounds are useful as intermediates for the synthesis of antibacterial agents.

Erythromycin A derivatives

Mucor circinelloides f. griseo-cyanus IFO 4563 is cultivated in a medium containing 6-O-methylerythromycin A as a substrate to obtain 14-hydroxy-6-O-methyl-erythromycin A. This compound and its salt have anti-bacterial activity.

Process for preparing 14-hydroxy-6-O-methyl-erythromycin A

Erythromycin derivatives represented by the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, R.sup.2 is a hydrogen atom or a hydroxy group, R.sup.3 is a hydrogen atom, a lower alkanoyl group, an alkoxycarbonyl group or an alkylsuccinyl group, and the salts thereof are disclosed. These compounds have antibacterial activity.

Erythromycin derivatives

A novel 6-O-methylerythromycin A derivative represented by the formula ##STR1## and the salts thereof are disclosed. These compounds are useful as intermediates for preparation of 6-O-methylerythromycin A and useful as antibiotics.

6-O-methylerythromycin a derivative

A method for the selective methylation of a hydroxy group at the 6-position of an erythromycin A derivative which comprises converting an erythromycin A derivative into an erythromycin A 9-oxime derivative, and reacting the resulting ethythromycin A 9-oxime derivative with an methylating agent.

Method for selective methylation of erythromycin A derivatives

Growing community of inventors

Saitama, Japan

Shigeo Morimoto