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1. 发明授权

US4358588A Process for preparing cephalosporanic acid compounds 失效
标题翻译：制备头孢菌素酸化合物的方法
公开(公告)号：US4358588A
公开(公告)日：1982-11-09
申请号：US193801
申请日：1980-10-03
申请人： Peter W. Henniger , Johannes K. van der Drift , Gerard J. van Veen , Jagdish C. Kapur
发明人： Peter W. Henniger , Johannes K. van der Drift , Gerard J. van Veen , Jagdish C. Kapur
IPC分类号： C07D499/12 , C07D20060101 , C07D499/00 , C07D499/64 , C07D499/68 , C07D501/06 , C07D501/20
CPC分类号： C07D499/00
摘要： A process for the preparation of [D-.alpha.-amino-p-hydroxyphenylacetamido]-penicillanic acid or cephalosporanic acid compounds comprising reacting a compound having a formula selected from the group consisting of ##STR1## wherein X is selected from the group consisting of hydrogen, acetoxy and five-membered heterocyclic group containing at least one hetero atom of the group consisting of oxygen, sulfur and nitrogen and optionally substituted with e.g. lower alkyl, this residue being attached to the 3-CH.sub.2 group via sulfur atom and wherein a NH radical if present has optionally been silylated with at least one mole equivalent of a silylating agent producing ##STR2## wherein R.sub.1, R.sub.2 and R.sub.3 are individually selected from the group consisting of lower alkyl, benzyl, cycloalkyl and phenyl in an inert anhydrous, organic solvent, preferably a water-inmiscible organic main-solvent, to form a compound having a formula selected from the group consisting of ##STR3## adjusting the pH to a scale value of 5.5 to 7.5 and reacting the resulting compounds in a pre-cooled solution with an at least equimolar amount of a compound of the formula wherein R.sub.4 is lower alkyl, R.sub.5 is selected from the group consisting of hydrogen and lower alkyl and R.sub.6 and R.sub.7 are lower alkoxy.
摘要翻译：一种制备[D-α-氨基 - 对 - 羟基苯基乙酰胺基] - 青霉烷酸或头孢菌酸化合物的方法，包括使具有选自以下的化合物：其中X是选自氢，乙酰氧基和含有至少一个由氧，硫和氮组成的组的杂原子的五元杂环基团，并且任选被例如低级烷基，该残基通过硫原子连接到3-CH 2基团，其中如果存在的话，NH基团任选用至少一摩尔当量的甲硅烷基化剂进行甲硅烷基化，产生其中R1，R2和R3被单独选择由低级烷基，苄基，环烷基和苯基组成的组在惰性无水的有机溶剂，优选与水不混溶的有机主要溶剂中形成具有选自以下的化合物：选自下组： IV将pH调节至5.5至7.5的比例值，并将所得化合物与预冷却的溶液与至少等摩尔量的下式化合物反应，其中R 4 是低级烷基，R 5选自氢和低级烷基，R 6和R 7是低级烷氧基。

2. 发明授权

US5266693A 6-diazo-penicillanic acid 1,1-dioxide derivatives 失效
标题翻译： 6-重氮 - 青霉烷酸1,1-二氧化物衍生物
公开(公告)号：US5266693A
公开(公告)日：1993-11-30
申请号：US880676
申请日：1992-05-08
申请人： Peter W. Henniger , Johannes K. van der Drift
发明人： Peter W. Henniger , Johannes K. van der Drift
IPC分类号： C07D499/00 , A61K31/425
CPC分类号： C07D499/00
摘要： A process for the preparation of at least one compound of a formula selected from the group consisting of ##STR1## and their salts and esters wherein X is selected from the group consisting of hydrogen and a substituent such as halogen and acetoxy comprising diazotizing a compound of the formula ##STR2## and salts and esters thereof wherein X has the above definition and brominating the resulting diazotized compound with at least an equimolar amount of a nitrosating agent in the presence of 1 to 5 equivalents of a strong acid in solution or suspension in a mixture of water and an at least partially water-miscible organic solvent with the amount of water being 1 to 20% by volume containing at least equimolar amounts of hydrogen bromide and bromine which bromo compounds are useful intermediates for the preparation of penicillanic acid-1,1-dioxide and its derivatives and novel 6-diazo-intermediates.
摘要翻译：一种制备至少一种选自下组的化合物的方法及其盐和酯，其中X选自氢和取代基，例如卤素和乙酰氧基，其包括使式III化合物及其盐和酯进行重氮化，其中X具有上述定义，并在至少等摩尔量的亚硝化剂的存在下，将所得重氮化化合物溴化为1至5当量的强在水和至少部分水混溶性有机溶剂的混合物中的溶液或悬浮液中的酸，其中水的量为1至20体积％，含有至少等摩尔量的溴化氢和溴。该溴化合物是用于制备青霉烷酸-1,1-二氧化物及其衍生物和新型6-重氮 - 中间体。

3. 发明授权

US4128547A 6-(D-.alpha.-Amino-p-hydroxyphenylacetamido)-penicillanic acid preparation 失效
标题翻译： 6-（D- {60-氨基 - 对羟基苯基乙酰氨基） - 青霉烷酸制剂
公开(公告)号：US4128547A
公开(公告)日：1978-12-05
申请号：US854821
申请日：1977-11-25
申请人： Johannes K. van der Drift , Peter W. Henniger , Gerard J. VAN Veen
发明人： Johannes K. van der Drift , Peter W. Henniger , Gerard J. VAN Veen
IPC分类号： C07D499/12 , C07D20060101 , C07D499/00 , C07D499/64 , C07D499/68 , C07D501/06 , C07D501/20 , C07D499/04
CPC分类号： C07D499/00
摘要： A process for the preparation of 6-(D-.alpha.-amino-p-hydroxyphenylacetamido)-penicillanic acid or amoxicillin by reacting 6-aminopenicillanic acid with at least two equivalents of a silylating agent producing trimethylsilyl groups in an anhydrous, inert, water-insoluble organic solvent and reacting the resulting product at a temperature below -25.degree. C with an at least equimolar amount of a compound of the formula ##STR1## wherein R.sub.1 and R.sub.7 are lower alkoxy, R.sub.2 is lower alkyl and R.sub.3 is selected from the group consisting of lower alkyl and hydrogen previously prepared from the corresponding Dane salt and an acid chloride under anhydrous conditions in the presence of a tertiary amine in an inert, water-insoluble organic solvent.
摘要翻译：通过使6-氨基青霉烷酸与至少两当量的产生三甲基甲硅烷基的甲硅烷基化试剂在无水，惰性，水溶液中制备6-（D-α-氨基 - 对羟基苯基乙酰胺基） - 青霉烷酸或阿莫西林的方法，使所得产物在低于-25℃的温度下与至少等摩尔量的式III化合物反应，其中R 1和R 7是低级烷氧基，R 2是低级烷基，R 3选自在惰性水不溶性有机溶剂中，在叔胺存在下，在无水条件下，由相应的丹烷盐和酰氯预先制备的低级烷基和氢原子组成的基团。

4. 发明授权

US4619786A Preparation of 6-.alpha.-bromo- and/or 6,6-dibromo-penicillanic acid-1,1-dioxides 失效
标题翻译： 6-溴 - 和/或6,6-二溴 - 青霉烷酸-1,1-二氧化物的制备
公开(公告)号：US4619786A
公开(公告)日：1986-10-28
申请号：US486981
申请日：1983-04-19
申请人： Peter W. Henniger , Johannes K. van der Drift
发明人： Peter W. Henniger , Johannes K. van der Drift
IPC分类号： C07D499/87 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/10 , C07D499/21 , C07D499/86 , C07D499/897 , C12N9/99 , A61K31/425
CPC分类号： C07D499/00
摘要： A process for the preparation of at least one compound of a formula selected from the group consisting of ##STR1## and their salts and esters wherein X is selected from the group consisting of hydrogen and a substituent such as halogen and acetoxy comprising diazotizing a compound of the formula ##STR2## and salts and esters thereof wherein X has the above definition and brominating the resulting diazotized compound with at least an equimolar amount of a nitrosating agent in the presence of 1 to 5 equivalents of a strong acid in solution or suspension in a mixture of water and an at least partially water-miscible organic solvent with the amount of water being 1 to 20% by volume containing at least equimolar amounts of hydrogen bromide and bromine which bromo compounds are useful intermediates for the preparation of penicillanic acid-1,1-dioxide and its derivatives and novel 6-diazo-intermediates.

5. 发明授权

US4528135A Process for the preparation of penicillanic acid 1,1-dioxides 失效
标题翻译：制备青霉烷酸1,1-二氧化物的方法
公开(公告)号：US4528135A
公开(公告)日：1985-07-09
申请号：US486403
申请日：1983-04-19
申请人： Peter W. Henniger , Johannes K. van der Drift , Jagdish C. Kapur , Herman P. Fasel
发明人： Peter W. Henniger , Johannes K. van der Drift , Jagdish C. Kapur , Herman P. Fasel
IPC分类号： C07D499/87 , A61K31/43 , A61P31/04 , C07D499/00 , C07D499/10 , C07D499/21 , C07D499/86 , C07D499/897 , C12N9/99
CPC分类号： C07D499/00
摘要： A process for the preparation of penicillanic acid-1,1-dioxides of the formula ##STR1## wherein X is selected from the group consisting of hydrogen and substituent such as halogen or acetoxy and R is selected from the group consisting of hydrogen, a pharmaceutically acceptable metal ion and/or ester radical comprising debrominating a 6-.alpha.-bromo- and/or 6,6-dibromo-penicillanic 1,1-dioxide selected from the group consisting of the formula ##STR2## wherein X and R have the above definition in an aqueous containing medium with zinc in association with an acid having a pK.sub.a -value measured in water less than 3.5 and optionally if R is H converting the acid into a pharmaceutically acceptable salt or ester.
摘要翻译：制备式II的青霉烷酸-1,1-二氧化物的方法，其中X选自氢和取代基如卤素或乙酰氧基，R选自氢，药学上可接受的金属离子和/或酯基，其包括将6-31-和6-或6-6-二溴 - 青霉烷状的1,1-二氧化物脱氟，所述6-8-溴 - 和/或6-6-二溴 - 青霉烷基1,1-二氧化物选自式III＆其中X和R在具有锌的含水介质中具有上述定义，其中锌与在水中测得的pKa值小于3.5并且任选地如果R是将酸转化成药学上可接受的盐或酯，

6. 发明授权

US4318852A Sodium amoxicillin solvate 失效
标题翻译：阿莫西林钠溶剂化物
公开(公告)号：US4318852A
公开(公告)日：1982-03-09
申请号：US257747
申请日：1981-04-27
申请人： Herwarth Heitman , Johannes K. van der Drift , Everardus J. A. M. Leenderts , Herman H. Grootveld
发明人： Herwarth Heitman , Johannes K. van der Drift , Everardus J. A. M. Leenderts , Herman H. Grootveld
IPC分类号： A61K31/43 , A61K47/00 , A61K47/22 , A61P31/04 , C07D499/04 , C07D499/22 , C07D499/26 , C07D499/68 , C07D499/893 , C07D499/897 , C07D499/44
CPC分类号： A61K9/0019 , A61K31/43 , A61K47/22
摘要： The solvate of sodium amoxicillin and N-methyl-2-pyrrolidone and its preparation which is a stable antibiotic from which injectable solutions may be prepared.
摘要翻译：阿莫西林钠和N-甲基-2-吡咯烷酮的溶剂合物及其制备方法，可制备可注射溶液的稳定抗生素。

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