Method of producing carbapenem derivatives

专利摘要:
A novel series of carbapenem derivatives characterized by a 2-substituent of the formula <IMAGE> in which n has a value of 1, 2 or 3; R5 represents an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroaraliphatic, heterocyclyl or heterocyclylaliphatic radical; and <IMAGE> represents a quaternized nitrogen-containing aromatic heterocycle bonded to the group -S-(CH2)n-S- via a ring carbon atom.
公开号:SU1614763A3
申请号:SU864028623
申请日:1986-11-21
公开日:1990-12-15
发明作者:Декстрейз Пьер
申请人:Бристоль Мейерз Сквибб Компани (Фирма)；
IPC主号:

专利说明:

where Ry is hydrogen or methyl;
Hs-cH, cH, -s-Qi
snSnz
I
I1
 OR
15
N COONa W.
characterized in that the compound of the general formula
15
where is the group
9Нз
SN
one
-O-ё | IAH1
.. N COOCH CH lH.i
in an inert solvent in the presence of a base, followed by removal of the protecting group Rg and, if necessary, methylation.

权利要求:
Claims (1)
[1]
Claim
The method of obtaining carbapenem derivatives of General formula
He to,
H ₃ C ^5CH 2 ^CH 2 ⁵ - £ ν
—Νΐτοθ '
ten
₀ ΧΐΧ
gde k
has the indicated meanings; alkyl or p-nitrobenzyl, is reacted with diphenyl chlorophosphate and the resulting product втη vCi pb is reacted with thiol of the general formula
where is hydrogen or methyl;
NZ-CH ₂ CH ₂ -8- £ s
Group
CH '
CH '
15
where is the group
θ '* or-C
COOH SND ²⁰
<ί ^Η 3 NGE or
coaxially ₇ sn = sn _g
characterized in that the compound of the general formula
in an inert solvent in the presence of a base, followed by the removal of the protective group K ₂ and, if necessary, by methylation.
Microorganisms Minimum µg / ml inhibitory concentrationin conjunction 1a....... ”G Imipenem A9585 0.001 0.016 0.001 A9604 0.001 0.016 0.001 A20688 0.130 8,000 0,250 A9537 0,004 0.030 0,002 0,008 0.130 0,008 0,004 1, 000 0.908 125,000 32,000 A15119 0,008 0.016 0,008 A20341 0.016 0.030 0.016 A9664 0.030 0.060 0.060 A20468 0.060 0.130 0.060 A9659 0.060 0.130 0.060 A9656 0.130 0.130 0.030 A9900 0.016 0.030 0,008 A21559 0.016 0.030 0.016 A15153 0.060 0.130 0.060 A22424 0.130 0,250 0.130 A20019 0.030 0.060 0.030 A9843 8,000 16,000 0,500 2,000 63,000 2,000

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引用文献:

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公开号 | 申请日 | 公开日 | 申请人 | 专利标题

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US4376774A|1979-05-29|1983-03-15|Merck & Co., Inc.|Antibiotic N-heterocyclyl thienamycin|

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FR2921382B1|2007-09-21|2009-10-30|Oreal|PHENYL-PYRIDOL [1,2-A] INDOLIUM THIOL-DISULFIDE DERIVATIVE DYE, TINCTORIAL COMPOSITION COMPRISING THE DYE, METHOD OF CLEANING KERATINIC MATERIALS FROM THAT COLORANT|

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法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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US06/800,867|US4880922A|1985-11-22|1985-11-22|Carbapenems with quaternized heterothioalkylthio substitution at position 2|

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