Sanraku Incorporated

Azuma Watanabe

Takeo Yoshioka

Yasuo Fukagawa

Tomoyuki Ishikura

Noritaka Chida

Rokuro Okamoto

Hiroshi Tone

Tomio Takeuchi

Tsutomu Sawa

Kaichiro Kominato

Hiroyuki Chiba

Kohki Kiyoshima

Koichiro Kominato

An angolamycin derivative represented by the following formula ##STR1## wherein X represents an acetyl, methanesulfonyl, methylthio, benzoyl or methoxy group. This compound is useful as a medicament such as antibacterial agent and an animal feed additive.

Angolamycin derivatives

A compound represented by the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group; R.sub.2 represents a lower alkyl group, a lower haloalkyl group, an aralkyl group, or a group of the formula --COOR.sub.4 or --SO.sub.2 R.sub.5 in which R.sub.4 represents an aralkyl group or a substituted or unsubstituted alkyl group and R.sub.5 represents an alkyl group or a substituted or unsubstituted aryl group; and R.sub.3 represents a hydrogen atom or a carboxyl protecting group which can be easily split off. This compound is useful in the production of a 6-(disubstituted amino)carbapenem-series antibiotic. The compounds of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as defined above are important intermediates for the synthesis of the compounds of formula (I) and/or the aforesaid di-(substituted amino) carbapenem-series antibiotics.

6-(disubstituted amino)carbapenem compounds

Tylosin derivatives represented by the following general formula (I): ##STR1## [wherein R denotes a hydrogen atom, acetyl, propionyl or a radical of Si(R.sup.2).sub.3 (in which R.sup.2 is a lower alkyl group), and R.sup.1 stands for a hydrogen atom or a radical of Si(R.sup.2 .sub.3 ] are useful as intermediates for the synthesis of 4'-acyl derivatives of tylosin because, after introduction of any desired acyl group at the 4'-hydroxyl group, the silyl protective group can be readily removed without liberation of the acyl group. This invention also provides processes for producing the tylosin derivatives. More specifically, it provides a melthod of selectively protecting 2'- and 4''-hydroxyl groups of tylosin (those of higher reactivity among the hydroxyl groups involved); a method of selectively protecting only the 4''-hydroxyl group of tylosin; a method of selectively protecting the 3- and 4''-hydroxyl groups of 2'-O-acyltylosin; and a method of protecting 3-, 2'- and 4''-hydroxyl groups of tylosin.

Tylosin derivatives and processes for producing the same

A compound represented by the formula ##STR1## wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group; R.sub.2 represents a lower alkyl group, a lower haloalkyl group, an aralkyl group, or a group of the formula --COOR.sub.4 or --SO.sub.2 R.sub.5 in which R.sub.4 represents an alkyl group or a substituted or unsubstituted aralkyl group and R.sub.5 represents an alkyl group or a substituted or unsubstituted aryl group; and R.sub.3 represents a hydrogen atom or a carboxyl protecting group which can be easily split off. This compound is useful in the production of a 6-(disubstituted amino)carbapenem-series antibiotic.

6-(disubstituted amino)carbapenam compounds

An azetidinone derivative of the formula ##STR1## wherein R.sub.1 represents a formyl group, a carboxyl group, an acetyloxy group or a group of the formula ##STR2## in which R.sub.2 and R.sub.3 each represent a lower alkyl group or together represent a lower alkylene group, and Z represents a hydrogen atom or an amino-protecting group.

Growing community of inventors

Fujisawa, Japan

Azuma Watanabe