Taisho Pharmaceutical Co., Ltd.

Jozi Nakagami

Kaoru Sota

Tadashi Eguchi

Yoshiaki Watanabe

Takashi Adachi

Shigeo Morimoto

Toshifumi Asaka

Takehiro Amano

Jiro Sawada

Yoshiaki Kamano

Masami Goi

Morihiro Mitsukuchi

Jinsaku Sakakibara

Yoshihiro Migita

Yukinari Kumazawa

Kazuhiko Michishita

Yasuhide Tachi

Mitsunori Washitake

Novel benzo[.alpha.]phenazine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, methyl, hydroxyl or alkoxy, R.sup.2 is --COOR.sup.5 (wherein R.sup.5 is hydrogen, straight or branched chain alkyl, cycloalkyl having 3-6 carbon atoms, benzyl or phenyl) or ##STR2## wherein R.sup.6 and R.sup.7 are the same or different and are each hydrogen or lower alkyl, or R.sup.6 and R.sup.7 together with the nitrogen atom to which they are attached form pyrrolidine or piperidine), R.sup.3 and R.sup.4 are the same or different and are each hydrogen or lower alkyl, and n is an integer of 2 or 3, and the salts thereof are disclosed. These compounds have antitumor activity in mammals.

Benzo[.alpha.]phenazine antitumor agents

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

17.alpha.-butyryloxy-11.beta.-hydroxy-21-propionyloxy-4-pregnen-3,20-dione, i.e., hydrocortisone 17-butyrate 21-propionate of the present invention is prepared by acylating hydrocortisone 17-butyrate with propionic acid anhydride or halide. The compound of the present invention has excellent anti-inflammatory effect, percutaneous absorption and less side effect.

Novel hydrocortisone derivative

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Ina, Japan

Jozi Nakagami