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11. 发明授权

US6096883A 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones 有权
标题翻译：基于3-羟基γ-内酯的对映选择性合成氮杂环丁酮
公开(公告)号：US6096883A
公开(公告)日：2000-08-01
申请号：US210921
申请日：1998-12-14
申请人： George G. Wu , Xing Chen , Yee-Shing Wong , Doris P. Schumacher , Martin Steinman
发明人： George G. Wu , Xing Chen , Yee-Shing Wong , Doris P. Schumacher , Martin Steinman
IPC分类号： C07D205/08
CPC分类号： C07D205/08
摘要： The invention relates to intermediates of the formulae ##STR1## said intermediates being useful in a process for producing a compound of the formula ##STR2## wherein Bn is benzyl and R.sub.1, .sub.2 and R.sub.3 are as defined in the specification,
摘要翻译：本发明涉及式的中间体，所述中间体可用于制备下式化合物的方法，其中Bn是苄基，R1,2和R3如说明书中所定义，

12. 发明授权

US5053502A Anhydro penicillin derivatives 失效
标题翻译：脱氢青霉素衍生物
公开(公告)号：US5053502A
公开(公告)日：1991-10-01
申请号：US524185
申请日：1990-05-15
申请人： Donald Hou , Yee-Shing Wong , Dinesh Gala , Martin Steinman
发明人： Donald Hou , Yee-Shing Wong , Dinesh Gala , Martin Steinman
IPC分类号： C07D205/09 , C07D499/88 , C07F7/18
CPC分类号： C07D499/88 , C07D205/09 , C07F7/186 , Y02P20/55
摘要： There is disclosed a compound represented by the formula ##STR1## where P is a hydroxy protecting group.
摘要翻译：公开了由式“IMAGE”表示的化合物，其中P是羟基保护基。

13. 发明授权

US4948885A Synthesis of azetidinones 失效
标题翻译：氮杂环丁酮的合成
公开(公告)号：US4948885A
公开(公告)日：1990-08-14
申请号：US370520
申请日：1989-06-23
申请人： Donald Hou , Yee-Shing Wong , Dinesh Gala , Martin Steinman
发明人： Donald Hou , Yee-Shing Wong , Dinesh Gala , Martin Steinman
IPC分类号： C07D205/09 , C07D499/88 , C07F7/18
CPC分类号： C07D499/88 , C07D205/09 , C07F7/186 , Y02P20/55
摘要： There is disclosed a compound represented by the formula ##STR1## wherein each P is hydrogen or a hydroxy protecting group and R and R' are each the same and are hydrogen, ##STR2## wherein R" is lower alkyl and R'" is a carboxy protecting group. The compounds are useful as intermediates for preparing penems.
摘要翻译：公开了由下式表示的化合物：其中每个P是氢或羟基保护基，R和R'各自相同并且是氢，其中R“是低级烷基，R”' 是羧基保护基。这些化合物可用作制备青铜的中间体。

14. 发明授权

US4554103A Preparation of 4-acyloxyazetidinones from acyl nitrates and penams 失效
标题翻译：由酰基硝酸盐和阴茎制备4-酰氧基氮杂环丁酮
公开(公告)号：US4554103A
公开(公告)日：1985-11-19
申请号：US513887
申请日：1983-07-14
申请人： Martin Steinman , Yee-Shing Wong
发明人： Martin Steinman , Yee-Shing Wong
IPC分类号： C07D205/08 , C07D499/88
CPC分类号： C07D205/08 , C07D499/88
摘要： There is disclosed a high yielding process for cleaving penicillinates with acyl or aroyl nitrates to produce acyloxy or aroyloxy azetidinones which are intermediates in the multistep process for producing penems from penicillinates.
摘要翻译：公开了一种用酰基或硝酸芳酯裂解青霉素的高产率方法，以产生酰基氧基或芳酰氧基氮杂环丁酮，它们是在从青霉菌生产青霉素的多步骤过程中的中间体。

15. 发明授权

US5886171A 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones 失效
标题翻译：基于3-羟基γ-内酯的对映选择性合成氮杂环丁酮
公开(公告)号：US5886171A
公开(公告)日：1999-03-23
申请号：US864529
申请日：1997-05-28
申请人： Guang-Zhong Wu , Xing Chen , Yee-Shing Wong , Doris P. Schumacher , Martin Steinman
发明人： Guang-Zhong Wu , Xing Chen , Yee-Shing Wong , Doris P. Schumacher , Martin Steinman
IPC分类号： C07D205/08
CPC分类号： C07D205/08
摘要： The invention relates to a process for producing a compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which comprises the steps of: (a) reacting a lactone with an imine to obtain a chiral diol of the formula IV; (b) oxidizing the diol to obtain an aldehyde of formula V; (c) condensing the aldehyde with an enolether followed by dehydration to obtain a compound of formula VI; (d) hydrogenating the compound of formula VI to obtain a ketone of formula VII; and (e) chirally catalytically reducing the ketone, wherein steps (b)-(d) are shown in the following reaction scheme: ##STR2##
摘要翻译：本发明涉及一种制备下式化合物的方法，其中R 1，R 2和R 3如说明书中所定义，其包括以下步骤：（a）使内酯与亚胺反应，得到手性二醇公式IV; （b）氧化二醇以获得式V的醛; （c）将醛与烯醇缩合，然后脱水得到式VI化合物; （d）使式Ⅵ化合物氢化得到式Ⅶ的酮; 和（e）手性催化还原酮，其中步骤（b） - （d）显示在以下反应方案中：

16. 发明授权

US4876338A Synthesis of azetidinones using CuCl 失效
标题翻译：使用CuCl合成氮杂环丁酮
公开(公告)号：US4876338A
公开(公告)日：1989-10-24
申请号：US203385
申请日：1988-06-07
申请人： Donald Hou , Yee-Shing Wong , Dinesh Gala , Martin Steinman
发明人： Donald Hou , Yee-Shing Wong , Dinesh Gala , Martin Steinman
IPC分类号： C07D205/09 , C07D499/88 , C07F7/18
CPC分类号： C07F7/186 , C07D205/09 , C07D499/88 , Y02P20/55
摘要： A multi-step stereospecific process for preparing (3S,4R,5R)-1-(allyloxycarbonyl)-methyl-3-(1-hydroxyethyl)-4-beta-naphthoxythi ocarbonylthio-2-azetidinone, stereoisomers thereof or hydroxy protected analogs thereof from anhydropenicillin. The azetidinones are intermediates useful for producing penems which are a known group or antibacterial compounds. The process involves protecting the hydroxy group of anhydropenicillin with a readily removable hydroxy protecting group, then reacting the resulting compound by treatment with oxygen and cuprous chloride in methanol, followed by reaction with ozone to produce a hydroxy protected dithiobis azetidinone and convert the methylidene groups originally in the 2-position of anhydropenicillin and in the bis-compound, to a (methoxycarbonyl)-carbonyl group. The resulting compound is converted to the unprotected dithiobis compound by reaction with ammonium hydroxide, then allyliodoacetate followed by an acid. Reaction of the resulting compound with zinc and a mineral acid followed by reaction with 0-2-naphthalenylcarbonochloridothioate converts the unprotected dithiobis compound to 1-(allyloxycarbonyl)methyl-3-(1-hydroxyethyl)-4-beta-naphthoxy (thiocarbonyl)thio-2-azetidinone.
摘要翻译：制备（3S，4R，5R）-1-（烯丙氧基羰基） - 甲基-3-（1-羟乙基）-4-β-羟基硫羰硫基-2-氮杂环丁酮的多步立体选择性方法，其立体异构体或羟基保护的类似物来自脱水青霉素。氮杂环丁酮是可用于生产作为已知组或抗菌化合物的青霉烯的中间体。该方法包括用易于除去的羟基保护基保护脱水青霉素的羟基，然后通过用甲醇中的氧和氯化亚铜处理使所得化合物反应，然后与臭氧反应，产生羟基保护的二硫代双环氮杂环丁酮并原来转化亚甲基在二氢化青霉素的2-位和双 - 化合物中的至（甲氧基羰基） - 羰基。所得化合物通过与氢氧化铵反应而转化为未保护的二硫代双酚化合物，然后与烯丙基碘乙酸酯反应，然后与酸反应。将所得化合物与锌和无机酸反应，然后与0-2-萘基碳氯化硫代磷酸酯反应，将未保护的二硫代双环化合物转化为1-（烯丙氧基羰基）甲基-3-（1-羟乙基）-4-β-萘氧基（硫代羰基）硫代 -2-氮杂环丁酮。

17. 发明授权

US5739321A 3-hydroxy .gamma.-lactone based enantionselective synthesis of azetidinones 失效
标题翻译：基于3-羟基γ-内酯的对映选择性合成氮杂环丁酮
公开(公告)号：US5739321A
公开(公告)日：1998-04-14
申请号：US655785
申请日：1996-05-31
申请人： Guang-Zhong Wu , Xing Chen , Yee-Shing Wong , Doris P. Schumacher , Martin Steinman
发明人： Guang-Zhong Wu , Xing Chen , Yee-Shing Wong , Doris P. Schumacher , Martin Steinman
IPC分类号： C07D205/08 , C07D205/04
CPC分类号： C07D205/08
摘要： The invention relates to a process for producing the compound of the formula ##STR1## which comprises reacting lactone of formula II ##STR2## with an imine of formula III': ##STR3## and converting the resulting chiral diol of formula VI: ##STR4## through several steps to obtain a compound of formula I'.
摘要翻译：本发明涉及制备式I的化合物的方法，其包括使式II的内酯与式III'的亚胺反应，并转化得到的式VI的手性二醇：通过几步来获得式I'化合物。

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