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US4990602A
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Erythromycin A derivatives
Assignee: Taisho Pharmaceutical Co Ltd
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Filing: 1988-12-12
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Granted: 1991-02-05
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Expires: 2008-12-12
Abstract
Abstract Erthromycin A derivatives represented by the general formula ##STR1## wherein R 1 is a group of the formula R 7 CH 2 -- (wherein R 7 is a hydrogen group or a lower alkyl group) or a group of the formula R 8 O-- (wherein R 8 is a lower alkyl group), R 2 is R 8 , a cycloalkyl group, a phenyl group or an aralkyl group.), or R 2 and R 7 together form an alkylene group, R 3 is a hydrogen atom, a lower alkyl group, a phenyl group or an aralkyl group, or R 3 and R 7 together form an alkylene group, or R 2 and R 3 together form an alkylene group, R 4 is a lower alkyl group, R 5 is a substituted silyl group, and R 6 is a hydrogen atom or R 5 , are disclosed. These compounds are useful as intermediates for the synthesis of antibacterial agents.
Inventors
- 👤 Shigeo Morimoto
- 👤 Takashi Adachi
- 👤 Tohru Matsunaga
- 👤 Masato Kashimura
- 👤 Toshifumi Asaka
- 👤 Yoshiaki Watanabe
- 👤 Kaoru Sota
- 👤 Kazuto Sekiuchi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 17:42
CPC Classifications
C; C07; C07H; C07H17/00; C07H17/04; C07H17/08
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
307 words
An Erythromycin A derivative represented by the formula: ##STR17## wherein R' is a group of the formula R 7 CH 2 -- (wherein R 7 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms) or a group of the formula R 8 O (wherein R 8 is an alkyl group having 1 to 6 carbon atoms), R 2 is R 8 , a cycloalkyl group having 5 to 7 carbon atoms, a phenyl group or an aralkyl group, or R 2 and R 7 together form an alkylene group having 2 or 3 carbon atoms, R 3 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a phenyl group or an aralkyl group, or R 3 and R 7 together form an alkylene group having 3 to 5 carbon atoms or an alkylene group having 3 to 5 carbon atoms and substituted by 1 to 3 alkyl groups having each 1 to 3 carbon atoms, or R 2 and R 3 together form an alkylene group having 3 or 4 carbon atoms, R 4 is an alkyl group having 1 to 3 carbon atoms, R 5 is a substituted silyl group of formula --SiR 9 R 10 R 11 (wherein R 9 , R 10 and R 11 are the same or different, and each is a hydrogen atom, an alkyl group having 1 to 15 carbon atoms, a phenyl substituted alkyl group in which the alkyl moiety has 1 to 3 carbon atoms, a phenyl group, a cycloalkyl group having 5 to 7 carbon atoms or an alkenyl group having 2 to 5 carbon atoms, with the proviso that at least one of R 9 , R 10 and R 11 is other than hydrogen atom), and R 6 is a hydrogen atom or R 5 .
Claim 2
Dependent Claim
307 words
An Erythromycin A derivative represented by the formula: ##STR17## wherein R' is a group of the formula R 7 CH 2 -- (wherein R 7 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms) or a group of the formula R 8 O (wherein R 8 is an alkyl group having 1 to 6 carbon atoms), R 2 is R 8 , a cycloalkyl group having 5 to 7 carbon atoms, a phenyl group or an aralkyl group, or R 2 and R 7 together form an alkylene group having 2 or 3 carbon atoms, R 3 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a phenyl group or an aralkyl group, or R 3 and R 7 together form an alkylene group having 3 to 5 carbon atoms or an alkylene group having 3 to 5 carbon atoms and substituted by 1 to 3 alkyl groups having each 1 to 3 carbon atoms, or R 2 and R 3 together form an alkylene group having 3 or 4 carbon atoms, R 4 is an alkyl group having 1 to 3 carbon atoms, R 5 is a substituted silyl group of formula --SiR 9 R 10 R 11 (wherein R 9 , R 10 and R 11 are the same or different, and each is a hydrogen atom, an alkyl group having 1 to 15 carbon atoms, a phenyl substituted alkyl group in which the alkyl moiety has 1 to 3 carbon atoms, a phenyl group, a cycloalkyl group having 5 to 7 carbon atoms or an alkenyl group having 2 to 5 carbon atoms, with the proviso that at least one of R 9 , R 10 and R 11 is other than hydrogen atom), and R 6 is a hydrogen atom or R 5 .
Claim 3
Dependent Claim
296 words
An Erythromycin A derivative represented by the formula: ##STR18## wherein R 1 is a group of the formula R 7 CH 2 -- (wherein R 7 is a hydrogen atom of an alkyl group having 1 to 3 carbon atoms) or a group of the formula R 8 O-- (wherein R 8 is an alkyl group having 1 to 6 carbon atoms), R 2 is R 8 , a cycloalkyl group having 5 to 7 carbon atoms, a phenyl group or an aralkyl group, or R 2 and R 7 together form an alkylene group having 2 or 3 carbon atoms, R 3 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a phenyl group or an aralkyl group, or R 3 and R 7 together form an alkylene group having 3 to 5 carbon atoms or an alkylene group having 3 to 5 carbon atoms and substituted by 1 to 3 alkyl groups having each 1 to 3 carbon atoms, or R 2 and R 3 together form an alkylene group having 3 or 4 carbon atoms, R 5 is a substituted silyl group of formula --SiR 9 R 10 R 11 (wherein R 9 , R 10 and R 11 are the same or different, and each is a hydrogen atom, an alkyl group having 1 to 15 carbon atoms, a phenyl substituted alkyl group in which the alkyl moiety has 1 to 3 carbon atoms, a phenyl group, a cycloalkyl group having 5 to 7 carbon atoms or an alkenyl group having 2 to 5 carbon atoms, with the proviso that at least one of R 9 , R 10 and R 11 is other than hydrogen atom), and R 6 is a hydrogen atom or R 5 .
Claim 4
Dependent Claim
296 words
An Erythromycin A derivative represented by the formula: ##STR18## wherein R 1 is a group of the formula R 7 CH 2 -- (wherein R 7 is a hydrogen atom of an alkyl group having 1 to 3 carbon atoms) or a group of the formula R 8 O-- (wherein R 8 is an alkyl group having 1 to 6 carbon atoms), R 2 is R 8 , a cycloalkyl group having 5 to 7 carbon atoms, a phenyl group or an aralkyl group, or R 2 and R 7 together form an alkylene group having 2 or 3 carbon atoms, R 3 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, a phenyl group or an aralkyl group, or R 3 and R 7 together form an alkylene group having 3 to 5 carbon atoms or an alkylene group having 3 to 5 carbon atoms and substituted by 1 to 3 alkyl groups having each 1 to 3 carbon atoms, or R 2 and R 3 together form an alkylene group having 3 or 4 carbon atoms, R 5 is a substituted silyl group of formula --SiR 9 R 10 R 11 (wherein R 9 , R 10 and R 11 are the same or different, and each is a hydrogen atom, an alkyl group having 1 to 15 carbon atoms, a phenyl substituted alkyl group in which the alkyl moiety has 1 to 3 carbon atoms, a phenyl group, a cycloalkyl group having 5 to 7 carbon atoms or an alkenyl group having 2 to 5 carbon atoms, with the proviso that at least one of R 9 , R 10 and R 11 is other than hydrogen atom), and R 6 is a hydrogen atom or R 5 .
Claim 5
Dependent Claim
3 words
2',4"-O-bis(trimethylsilyl)-erythromycin A 9-{O-[1-(1-methylethoxy)cyclohexyl]oxime}.
Claim 6
Dependent Claim
3 words
2',4"-O-bis(trimethylsilyl)-erythromycin A 9-{O-[1-(1-methylethoxy)cyclohexyl]oxime}.
References Cited (Backward Citations)
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