Patent EP0260938A2 successfully refreshed from Google Patents.
EP0260938A2
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EP
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Erythromycin A derivatives and method for preparing the same
Assignee: Taisho Pharmaceutical Co Ltd
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Filing: 1987-09-16
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Granted: —
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Expires: 2007-09-16
Abstract
Abstract Erythromycin A derivatives represented by the general formula <CHEM> wherein R<1> is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 groups selected from a halogen atom, an alkoxy group having 1 to 4 carbon atoms, a nitro group and an alkoxycarbonyl group having 2 to 6 carbon atoms, R<2> is a substituted silyl group and R<3> is a hydrogen atom or R<2>, are useful as intermediates for producing anti-bacterial agents.
Inventors
- 👤 Shigeo Morimoto
- 👤 Takashi Adachi
- 👤 Tohru Matsunaga
- 👤 Masato Kashimura
- 👤 Yoshiaki Watanabe
- 👤 Kaoru Sota
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-09 07:13
CPC Classifications
C; C07; C07H; C07H17/00; C07H17/04; C07H17/08
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
163 words
A 6-O-methylerythromycin A derivative represented by the general formula wherein R¹ is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 members selected from the group consisting of a halogen atom, an alkoxy group having 1 to 4 carbon atoms, a nitro group and an alkoxycarbonyl group having 2 to 6 carbon atoms, R² is a substituted silyl group of formula -SiR⁴R⁵R⁶ (wherein R⁴, R⁵ and R⁶ 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 R⁴, R⁵ and R⁶ is other than a hydrogen atom) and R³ is a hydrogen atom or R².
Claim 2
Dependent Claim
163 words
A 6-O-methylerythromycin A derivative represented by the general formula wherein R¹ is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 members selected from the group consisting of a halogen atom, an alkoxy group having 1 to 4 carbon atoms, a nitro group and an alkoxycarbonyl group having 2 to 6 carbon atoms, R² is a substituted silyl group of formula -SiR⁴R⁵R⁶ (wherein R⁴, R⁵ and R⁶ 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 R⁴, R⁵ and R⁶ is other than a hydrogen atom) and R³ is a hydrogen atom or R².
Claim 3
Dependent Claim
172 words
An erythromycin A derivative represented by the general formula wherein R¹ is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group or an arylmethyl group substituted by 1 to 3 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group and an alkoxycarbonyl group having 2 to 6 carbon atoms, R² is a substituted silyl group of formula -SiR⁴R⁵R⁶ (wherein R⁴, R⁵ and R⁶ 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 R⁴, R⁵ and R⁶ is other than a hydrogen atom) and R³ is a hydrogen atom or R².
Claim 4
Dependent Claim
172 words
An erythromycin A derivative represented by the general formula wherein R¹ is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group or an arylmethyl group substituted by 1 to 3 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group and an alkoxycarbonyl group having 2 to 6 carbon atoms, R² is a substituted silyl group of formula -SiR⁴R⁵R⁶ (wherein R⁴, R⁵ and R⁶ 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 R⁴, R⁵ and R⁶ is other than a hydrogen atom) and R³ is a hydrogen atom or R².
Claim 5
Independent Claim
231 words
A method for preparing a 6-O-methylerythromycin A derivative represented by the general formula wherein R¹ is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 members selected from the group consisting of a halogen atom, an alkoxy group having 1 to 4 carbon atoms, a nitro group and an alkoxycarbonyl group having 2 to 6 carbon atoms, R² is a substituted silyl group of formula -SiR⁴R⁵R⁶ (wherein R⁴, R⁵ and R⁶ 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 R⁴, R⁵ and R⁶ is other than hydrogen atom) and R³ is a hydrogen atom or R², which comprises reacting, in any desired sequence, erythromycin A 9-oxime with a compound of formula R¹-X (wherein R¹ is as defined above, and X is a halogen atom) and with a substituted silylating agent having R² group to give a compound represented by the general formula wherein R¹, R² and R³ are as defined above), and then reacting the resulting compound with a methylating agent.
Claim 6
Independent Claim
231 words
A method for preparing a 6-O-methylerythromycin A derivative represented by the general formula wherein R¹ is a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 members selected from the group consisting of a halogen atom, an alkoxy group having 1 to 4 carbon atoms, a nitro group and an alkoxycarbonyl group having 2 to 6 carbon atoms, R² is a substituted silyl group of formula -SiR⁴R⁵R⁶ (wherein R⁴, R⁵ and R⁶ 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 R⁴, R⁵ and R⁶ is other than hydrogen atom) and R³ is a hydrogen atom or R², which comprises reacting, in any desired sequence, erythromycin A 9-oxime with a compound of formula R¹-X (wherein R¹ is as defined above, and X is a halogen atom) and with a substituted silylating agent having R² group to give a compound represented by the general formula wherein R¹, R² and R³ are as defined above), and then reacting the resulting compound with a methylating agent.
References Cited (Backward Citations)
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