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公开(公告)号：US4508921A
公开(公告)日：1985-04-02
申请号：US625761
申请日：1984-06-28
IPC分类号： C07D265/10 , C07C67/00 , C07C227/00 , C07C227/14 , C07C227/18 , C07C227/32 , C07C229/02 , C07D263/20 , C07C51/09
CPC分类号： C07C227/32 , C07D263/20 , Y02P20/55
摘要： A process for preparing .alpha.-alkyl amino acids by enantioretentive .alpha.-alkylation of .alpha.-amino acids is described. The products are bioactive compounds including some useful as therapeutic agents.
摘要翻译： 描述了通过α-氨基酸的对映异构α-烷基化制备α-烷基氨基酸的方法。 该产品是包括一些可用作治疗剂的生物活性化合物。
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公开(公告)号：USRE31429E
公开(公告)日：1983-10-25
申请号：US87603
申请日：1979-10-23
IPC分类号： C07D473/00 , C07D513/04
CPC分类号： C07D473/00 , C07D513/04
摘要： 9-(Dihalobenzyl)adenines are prepared uncontaminated with other positional isomers in a series of mild transformations starting from 4,5,6-triaminopyrimidine and proceeding via 7-(N-formyl-N-dihalobenzyl)amino[1,2,5]-thiadiazolo[3,4-d]pyrimidine. The resulting compounds have anticoccidial activity and are useful in controlling cecal and/or intestinal coccidiosis when administered in minor quantities to animals, in particular to poultry usually in admixture with animal sustenance.
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公开(公告)号：US4053286A
公开(公告)日：1977-10-11
申请号：US689408
申请日：1976-05-24
申请人： Leonard M. Weinstock
发明人： Leonard M. Weinstock
IPC分类号： C07D501/04 , C07D501/06
CPC分类号： C07D501/04 , C07D501/06
摘要： An improved process for preparing the compound 7.beta.-(2-thienylacetamido)-7-methoxy-3-carbamoyloxymethyl-3-cephem-4-carboxylic acid or its esters, from the compound 7.beta.-(D-5-amino-5-carboxyvaleramido)-3-carbamoyloxymethyl-7-methoxy-3-cephem-4-carboxylic acid, by conducting the transacylation of the latter compound in the presence of commercially available alumino-silicate zeolites, also known as "molecular sieves." The process can be employed to prepare a cephalosporin with a desired 7-acylamido group from cephalosporins having a broad range of different 7-acylamido groups without having to isolate and purify a 7-amino intermediate. The final products have utility as broad spectrum antibiotics.
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公开(公告)号：US4010173A
公开(公告)日：1977-03-01
申请号：US553185
申请日：1975-02-26
IPC分类号： C07D277/56 , C07D277/28
CPC分类号： C07D277/56
摘要： 4-Cyanothiazoles are prepared by reacting .beta.,.beta.-dichloro-.alpha.-amino-acrylonitrile with a thioformamide in the presence of an acidic catalyst.
摘要翻译： 通过使β，β-二氯-α-氨基 - 丙烯腈与硫代甲酰胺在酸性催化剂存在下反应来制备4-氰基噻唑。
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公开(公告)号：US3962338A
公开(公告)日：1976-06-08
申请号：US417301
申请日：1973-11-19
IPC分类号： C07C309/63 , C07D263/06 , C07D285/10 , C07C91/02 , C07C93/02 , C07C93/10 , C07C95/02
CPC分类号： C07D285/10 , C07C309/63 , C07D263/06
摘要： Preparation of an optically active alkamine in the sinister configuration, or a derivative of said alkamine, which is reacted with an 3-X-4-chloro(or RO-- where R is hydrogen or an alkali metal)-1,2,5-thiadiazole to prepare S-3-X-4-(3-substituted amino-2-hydroxypropoxy)-1,2,5-thiadiazole beta adrenergic blocking agents. Novel 3-morpholino-4-chloro(or RO--)-1,2,5-thiadiazoles and their preparation also are described.
摘要翻译： 制备呈阴性构型的光学活性烷胺或所述烷胺的衍生物，其与3-X-4-氯（或RO-，其中R为氢或碱金属） 噻吩并制备S-3-X-4-（3-取代氨基-2-羟基丙氧基）-1,2,5-噻二唑β肾上腺素能阻断剂。 还描述了新的3-吗啉代-4-氯（或RO - ） - 1,2,5-噻二唑及其制备方法。
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6.发明授权
公开(公告)号：US4362726A
公开(公告)日：1982-12-07
申请号：US257062
申请日：1981-04-24
IPC分类号： C07D285/10 , C07D413/04 , A61K31/425 , A61K31/535 , C07D417/04
CPC分类号： C07D285/10
摘要： Substituted-1,2,5-thiadiazole-1-oxides, their preparation and pharmaceutical use as elastase inhibitors are disclosed.
摘要翻译： 公开了取代的1,2,5-噻二唑-1-氧化物，它们的制备和药物用途作为弹性蛋白酶抑制剂。
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公开(公告)号：US4111948A
公开(公告)日：1978-09-05
申请号：US745517
申请日：1976-11-26
IPC分类号： C07D277/22 , C07D277/02
CPC分类号： C07D277/22
摘要： Process for desulfurization of thiazoles including the removal of the mercapto group from 2-mercaptothiazoles and 2-mercaptobenzothiazoles and their derivatives by the oxidation with oxygen in the presence of an oxidation catalyst.
摘要翻译： 包括通过在氧化催化剂存在下用氧氧化从2-巯基噻唑和2-巯基苯并噻唑及其衍生物中除去巯基的方法。
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8.发明授权
公开(公告)号：US3946009A
公开(公告)日：1976-03-23
申请号：US408032
申请日：1973-10-19
IPC分类号： C07D241/18 , C07D413/04 , C07D295/00
CPC分类号： C07D413/04 , C07D241/18 , Y10S514/821
摘要： 2-(3-Substituted amino-2-hydroxypropoxy)-3-substituted pyrazine compounds optionally having substituents in the 5 and/or 6 positions, possessing .beta.-adrenergic blocking properties are described. The products are prepared by reaction of a 2-chloro(or hydroxy)pyrazine with a 5-hydroxy-methyl(or sulfonyloxymethyl)oxazolidine followed by acid hydrolysis.
摘要翻译： 描述了具有β-肾上腺素能阻断性质的5-和/或6位任选具有取代基的2-（3-取代的氨基-2-羟基丙氧基）-3-取代的吡嗪化合物。 产物通过2-氯（或羟基）吡嗪与5-羟基 - 甲基（或磺酰氧基甲基）恶唑烷的反应然后酸水解反应制备。
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公开(公告)号：US4834846A
公开(公告)日：1989-05-30
申请号：US129496
申请日：1987-12-07
IPC分类号： C07D205/08 , C07D205/085 , C07D403/04 , C07F7/18
CPC分类号： C07D403/04 , C07D205/08 , C07D205/085 , C07F7/186
摘要： This invention relates to a process for preparing .beta.-lactams by electrochemically deblocking N-substituting .beta.-lactams using anodic oxidation.
摘要翻译： 本发明涉及通过使用阳极氧化电化学去除N-取代的β-内酰胺来制备β-内酰胺的方法。
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公开(公告)号：US4282364A
公开(公告)日：1981-08-04
申请号：US152281
申请日：1980-05-22
IPC分类号： C07D277/22
CPC分类号： C07D277/22
摘要： An improved process for the preparation of thiazoles is disclosed. The process utilizes a substituted imine and sulfur dioxide heated in the presence of a catalyst. The thiazoles are known important chemical intermediates.
摘要翻译： 公开了改进的制备噻唑的方法。 该方法利用在催化剂存在下加热的取代的亚胺和二氧化硫。 噻唑是已知的重要化学中间体。
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