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公开(公告)号：US3975385A
公开(公告)日：1976-08-17
申请号：US503274
申请日：1974-09-05
IPC分类号： C07D501/08 , C07D499/00 , C07D501/10 , C07D501/22
CPC分类号： C07D499/00
摘要： The invention provides 7-trichloroacetamido-3-desacetoxy-cephalosporanic acid derivatives of the formula: ##SPC1##Wherein R is a group which protects the carboxylic acid radical, which can be converted into 7-amino-3-desacetoxycephalosporanic acid by replacing the R-- and Cl.sub.3 C--CO-- radicals by hydrogen atoms.
摘要翻译： 本发明提供下式的7-三氯乙酰氨基-3-脱乙酸基 - 头孢烷酸衍生物：
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公开(公告)号：US3978078A
公开(公告)日：1976-08-31
申请号：US557095
申请日：1975-03-10
IPC分类号： C07D499/68 , C07D499/80
CPC分类号： C07D499/68 , C07D499/80
摘要： Ampicillin is prepared by reacting an inorganic or organic base with a new penicillin G derivative of the formula: ##EQU1## (wherein R.sub.1 represents a group protecting the carboxy radical and R.sub.2 represents a strong electron-attracting group, e.g. a halogenoethyl group) to open the imidazolidine ring and give an intermediate product of the formula: ##EQU2## and removing by methods known per se the groups --R.sub.1 and R.sub.2 O--CS-- which protect the carboxy radical and amine functions respectively.
摘要翻译： 氨苄青霉素通过使无机或有机碱与新的下式的青霉素G衍生物反应制备：OHS | ANGLE CH3 C6H5-CH2-C --- N ---- CH-CHC ANGLE |||| CH3 R2O-CS -NC = OO = CN --- CH-COOR1 ANGLE CH | C6H5（其中R1表示保护羧基的基团，R2表示强电子吸引基团，例如卤代乙基），以打开咪唑烷环，得到中间体 下式的产物：S ANGLE CH3 R2O-CS-NH-CH-CONH-CH-CHC ANGLE ||| CH3 C6H5O = CN --- CH-COOR1，通过本身已知的方法除去基团-R1和R2O -CS-分别保护羧基和胺官能团。
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3.发明授权.beta.-aminovinyl ketones, a preparation process and their use in the preparation of .beta.-diketones 失效β-氨基乙烯基酮，其制备方法及其在制备β-二酮中的应用
公开(公告)号：US5684206A
公开(公告)日：1997-11-04
申请号：US569266
申请日：1996-03-20
申请人： Michel Casado , Pierre Le Roy , Virginie Pevere
发明人： Michel Casado , Pierre Le Roy , Virginie Pevere
IPC分类号： B01J27/02 , B01J27/10 , C07B61/00 , C07C45/42 , C07C49/217 , C07C49/563 , C07C69/78 , C07C225/16 , C07C319/20 , C07C323/32 , C07C49/76
CPC分类号： C07C323/32 , C07C319/20 , C07C2101/02
摘要： Novel .beta.-aminovinyl ketones of the general formula ##STR1## wherein R.sup.1 is, in particular, an alkenyl, alkynyl, cycloalkyl or cycloalkenyl group; R.sup.2 is, in particular, an electron-attracting substituent such as nitro, acyl, ester, alkylthio, carbamoyl, thiocarbamoyl or haloalkyl; R.sup.3 is, in particular, an alkyl or alkoxy group or a halogen atom; n is 1 or 2 and m is 0, 1, 2 or 3. A method for preparing such compounds by carrying out a condensation reaction between ketone R.sup.1 --CO--CH.sub.3 and, in particular, benzonitrile substituted by (R.sup.2).sub.n and optionally (R.sup.3).sub.m, in the presence of a strong base, as well as a process employing said .beta.-aminovinyl ketones of general formula (VI) for preparing the corresponding .beta.-diketones, are also disclosed.
摘要翻译： PCT No.PCT / FR94 / 00726 Sec。 371日期：1996年3月20日 102（e）1996年3月20日PCT 1994年6月16日PCT公布。 公开号WO95 / 00476 日期1995年1月5日通式（VI）的新型β-氨基乙烯基酮其中R 1特别是烯基，炔基，环烷基或环烯基; R2特别是吸电子取代基如硝基，酰基，酯，烷硫基，氨基甲酰基，硫代氨基甲酰基或卤代烷基; R3特别是烷基或烷氧基或卤素原子; n为1或2，m为0,1,2或3.通过进行酮R1-CO-CH3之间的缩合反应，特别是被（R 2）n取代的苄腈和任选（ R3）m，在存在强碱的情况下，以及采用通式（VI）的β-氨基乙烯基酮制备相应的β-二酮的方法也被公开。
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4.发明申请公开(公告)号：US20060142614A1
公开(公告)日：2006-06-29
申请号：US10532160
申请日：2003-10-24
申请人： Bernard Buathier , Pierre Le Roy
发明人： Bernard Buathier , Pierre Le Roy
IPC分类号： C07C211/45
CPC分类号： C07C209/74 , C07C211/52
摘要： Process for the preparation of a compound of general formula (I): in which X represents a halogen atom, by reaction of para-trifluoromethylaniline of formula (II): with a dihalogen X2, the two compounds being introduced simultaneously into a polar aprotic solvent in a dihalogen/compound (II) molar ratio ranging from 1.9 to 2.5 and at a temperature ranging from 100 to 300° C.
摘要翻译： 制备通式（I）化合物的方法：其中X表示卤素原子，通过式（II）的对三氟甲基苯胺与二卤代X 2 H 2反应，将两种化合物 同时引入极性非质子溶剂中，二卤化物（II）摩尔比为1.9-2.5，温度为100-300℃。
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公开(公告)号：US4347359A
公开(公告)日：1982-08-31
申请号：US225446
申请日：1981-01-15
IPC分类号： C07D249/10 , C07D253/075 , C07D257/04 , C07D317/28 , C07D319/06 , C07D501/24 , C07D253/06
CPC分类号： C07D253/075 , C07D257/04 , C07D317/28 , C07D319/06
摘要： New thiols of the general formula: ##STR1## wherein A represents a 2-hydroxy-1-oxoethan-1-yl-2-ylidene or alkoxycarbonylmethyne radical or a nitrogen atom and R represents various substituted alkyl radicals, and their alkali metal and alkaline earth metal salts are useful as intermediates in the preparation of cephalosporins having anti-bacterial properties.
摘要翻译： 新的具有以下通式的硫醇：其中A代表2-羟基-1-氧代乙烷-1-基-2-亚基或烷氧基羰基甲炔基或氮原子，R代表各种取代的烷基，以及它们的碱金属和碱 地球金属盐可用作制备具有抗菌性质的头孢菌素的中间体。
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公开(公告)号：US4307230A
公开(公告)日：1981-12-22
申请号：US152084
申请日：1980-05-21
IPC分类号： C07D501/04 , A61K31/545 , A61K31/546 , A61P31/04 , C07D253/075 , C07D257/04 , C07D317/28 , C07D501/00 , C07D501/06 , C07D501/14 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/60
CPC分类号： C07D253/075 , C07D257/04 , C07D317/28 , C07D501/00 , C07D501/24
摘要： Novel 3-vinyl-cephalosporins of the formula ##STR1## in which n is 0 or 1, R.sub.1 is hydrogen, a radical of the formula ##STR2## [in which R.sub.4 is hydrogen or a protective radical and R.sub.5 is hydrogen, alkyl, vinyl or cyanomethyl or is a protective radical], or a protective radical, and R.sub.2 is hydrogen, a protective radical or an enzymatically removable radical, or R.sub.1 is hydrogen or an acyl radical which may carry various substituents and R.sub.2 is hydrogen or a protective radical, and R.sub.3 is a radical of the general formula R'.sub.3 --SO.sub.2 --O-- or R".sub.3 --CO--O--, in which R'.sub.3 is alkyl, trifluoromethyl, trichloromethyl or phenyl which is substituted by a halogen atom or by an alkyl or nitro radical, and R".sub.3 is defined like R'.sub.3 or represents methyl which is substituted by acyl or alkoxycarbonyl, or represents ethyl or propyl substituted in the 2-position by acyl or alkoxycarbonyl. These compounds are useful as intermediates for the preparation of antibiotic 3-thiovinyl-cephalosporins.
摘要翻译： 式（I）的新型3-乙烯基头孢菌素其中n为0或1，R 1为氢，式（II）的基团[其中R 4为氢或保护基，R 5为 是氢，烷基，乙烯基或氰基甲基，或是保护基]或保护基，R2是氢，保护基或酶可除去的基团，或R 1是氢或可以带有各种取代基的酰基，R 2是 氢或保护基，R3是通式为R'3-SO2-O-或R'3-CO-O-的基团，其中R'3是烷基，三氟甲基，三氯甲基或被取代的苯基 卤素原子或烷基或硝基，R“3定义为R'3，或表示被酰基或烷氧基羰基取代的甲基，或代表在2-位被酰基或烷氧基羰基取代的乙基或丙基。 这些化合物可用作制备抗生素3-硫代乙烯基 - 头孢菌素的中间体。
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公开(公告)号：US4960904A
公开(公告)日：1990-10-02
申请号：US403444
申请日：1989-09-06
IPC分类号： B01J23/46 , B01J27/13 , C07B61/00 , C07D327/10
CPC分类号： C07D327/10
摘要： Cyclic sulphates of formula: ##STR1## are prepared by oxidation of a cyclic sulphite of formula: ##STR2## with a hypohalite of an alkali or alkaline-earth metal and a catalytic quantity of a ruthernium derivative (RuO.sub.2, RuCl.sub.3). In formulae (I) and (II), R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are identical or different and each represents hydrogen, halogen, alkyl, alkoxy, aryl, aryloxy or alkoxycarbonyl.
摘要翻译： 式（I）的环硫酸盐通过用碱金属或碱土金属的次卤酸盐和催化量的铼衍生物（RuO 2， RuCl3）。 在式（I）和（II）中，R 1，R 2，R 3，R 4，R 5和R 6相同或不同，各自表示氢，卤素，烷基，烷氧基，芳基，芳氧基或烷氧基羰基。
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公开(公告)号：US4950784A
公开(公告)日：1990-08-21
申请号：US77239
申请日：1987-07-24
IPC分类号： C07F9/17
CPC分类号： C07F9/17
摘要： The O-alkyl S,S-dialkylphosphorodithioates, e.g., ethoprophos, are facilely prepared, in improved yields and having great purity, by reacting an alkylphosphate dihalogenide, e.g., a dichloride, with a 1.5 to 8 mol excess of a thiol, in the presence of a 0.1 to 5 mol excess of an acid acceptor, with both molar excesses being per mole of said dihalogenide.
摘要翻译： O-烷基S，S二烷基二硫代磷酸酯，例如鸟嘌呤，通过使二卤化烷基磷酸酯与1.5至8摩尔过量的硫醇反应，以提高产率和高纯度方便地制备， 存在0.1至5摩尔过量的酸受体，两摩尔过量是每摩尔所述二卤化物。
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公开(公告)号：US4554350A
公开(公告)日：1985-11-19
申请号：US522261
申请日：1983-08-11
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/24
CPC分类号： C07D501/24
摘要： New cephalosporin derivatives of the formula: ##STR1## in which R is an amino-protecting radical, R' is a protected carboxyl radical, Hal is a halogen atom, R.sub.a, R.sub.b and R.sub.c are hydrogen atoms, or R.sub.a is a protected carboxyl radical and R.sub.b and R.sub.c, which are identical or different, are hydrogen atoms, or C.sub.1 -C.sub.4 alkyl radicals, or together form a C.sub.2 -C.sub.5 alkylene radical, and n=0 or 1, their isomeric forms and mixtures thereof, are useful for the preparation of cephalosporins which have antibacterial properties.
摘要翻译： 下式的新型头孢菌素衍生物：其中R为氨基保护基，R'为被保护的羧基，Hal为卤素原子，Ra，Rb和Rc为氢原子，或Ra为被保护的羧基 和相同或不同的R b和R c是氢原子或C 1 -C 4烷基，或一起形成C 2 -C 5亚烷基，n = 0或1，它们的异构形式及其混合物可用于 制备具有抗菌性能的头孢菌素。
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公开(公告)号：US4369315A
公开(公告)日：1983-01-18
申请号：US323113
申请日：1981-11-19
IPC分类号： A61K31/535 , A61P31/04 , C07D501/24 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00
摘要： New oxacephalosporins of the general formula ##STR1## in which R.sub.1 is a protective radical and (a) R.sub.4 is a substituted 2-(2-aminothiazol-4-yl)-acetyl radical of which the amine group is protected, or an .alpha.-carboxyarylacetyl radical, and R" is hydrogen or methoxy in the 7.alpha.-position, or alternatively(b) R.sub.4 is a protective radical and R" is hydrogen or methoxy in the 7.alpha.-position or hydrogen in the 7.beta.-position, in the form of a bicyclooct-2-ene or bicyclooct-3-ene or a 3-oxoethylidenebicyclooctane, are useful as intermediates for the preparation of pharmaceutically active oxacephalosporins.
摘要翻译： 其中R 1为保护基的通式为（IMA）（Ⅰ）的新型硫代吗啡，（a）R4为被保护的胺基的取代的2-（2-氨基噻唑-4-基） - 乙酰基，或 一个α-羧基芳基乙酰基，R“是7个α-位的氢或甲氧基，或者（b）R4是保护基，R”是7位中的氢或甲氧基或7位中的氢 以双环-2-烯或双环辛烯-3-烯或3-氧代亚乙基双环辛烷的形式的β-位可用作制备药学活性的硫氰酸头孢菌素的中间体。
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