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    Process for intermediates to 1-carbapenems and 1-carbacephems
    6.
    发明授权
    Process for intermediates to 1-carbapenems and 1-carbacephems 失效
    1-碳青霉烯类和1-碳卡铂的中间体方法

    公开(公告)号：US4845229A

    公开(公告)日：1989-07-04

    申请号：US160801

    申请日：1988-02-26

    申请人： Chi-nung W. Hsiao ,  Marvin J. Miller

    发明人： Chi-nung W. Hsiao ,  Marvin J. Miller

    IPC分类号： C07D317/30 ,  C07D417/06 ,  C07F5/02

    CPC分类号： C07D417/06 ,  C07D317/30 ,  C07F5/025

    摘要： A stereoselective process for chiral intermediates to 1-carbapenem and 1-carbacephalosporins is provided comprising the use of an N-acyl-(4R)-substituted-1,3-thiazolidine-2-thione as a chiral auxiliary in boron enolate mediated aldol condensation with a protected-.beta.-keto ester aldehyde. E.g., benzyl 3,3-(ethylenedioxy)-4-formylbutyrate is condensed with the boron enolate formed with n-butyryl (4R)-methoxycarbonyl-1,3-thiazolidine-2-thione to provide benzyl 3,3-ethylenedioxy-(5R)-hydroxy-6-[(4R)-methoxycarbonyl-1,3-thiazolidine-2-thione-3-ylcarbonyl]octanoate. Displacement of the thiazolidine-2-thione chiral auxiliary moiety with an O-alkyl, O-acyl or O-aralkyl hydroxyamine provides the corresponding chiral intermediate as the hydroxamate.

    摘要翻译： 提供了一种用于1-碳青霉烯和1-碳头孢菌素的手性中间体的立体选择性方法，其包括在硼烯醇化物介导的醛醇缩合中使用N-酰基 - （4R） - 取代-1,3-噻唑烷-2-硫酮作为手性助剂 与保护的β-酮酯醛。 例如，3,3-（亚乙二氧基）-4-甲酰基丁酸苄酯与由正丁酰（4R） - 甲氧基羰基-1,3-噻唑烷-2-硫酮形成的硼烯醇化物缩合，得到3,3-亚乙二氧基 - （ 5R） - 羟基-6 - [（4R） - 甲氧基羰基-1,3-噻唑烷e-2-硫酮-3-基羰基]辛酸酯。 噻唑烷-2-硫酮手性辅助部分与O-烷基，O-酰基或O-芳烷基羟胺的位移提供相应的手性中间体作为异羟肟酸酯。

    Antimycobacterial agents
    7.
    发明授权
    Antimycobacterial agents 失效
    抗分枝杆菌药

    公开(公告)号：US06310058B1

    公开(公告)日：2001-10-30

    申请号：US09578973

    申请日：2000-05-25

    申请人： Marvin J. Miller ,  Yanping Xu

    发明人： Marvin J. Miller ,  Yanping Xu

    IPC分类号： A61K3155

    CPC分类号： C07D403/12 ,  C07D413/12

    摘要： Compounds represented by the formula [1] R1 is H or a substituent; R2 and R3 are C1-C3 alkyl; R4 is siderophore group e.g. CH3—(CH2)n—C(O)—N(OH)—(CH2)m— with n=10-22, m=2-6; X is O, S, or NH; X1 is O or NH; Y is H or alkyl; Z is H or substituted amino, e.g., t-BocNH or CbzNH, and r is 2-4; are useful in the method provided for treating tuberculosis. [1] is prepared by coupling [7], wherein HX1 is HO— or H2N—,  with [4] obtained as the free acid after saponification of the methyl ester.

    摘要翻译： 由式[1] R 1表示的化合物是H或取代基; R2和R3是C1-C3烷基; R4是铁载体基团 CH 3 - （CH 2）n -C（O）-N（OH） - （CH 2）m - ，其中n = 10-22，m = 2-6; X是O，S或NH; X1是O或NH; Y是H或烷基; Z是H或取代的氨基，例如t-BocNH或CbzNH，r是2-4; 可用于治疗结核病的方法。 [1]通过偶联[7]制备，其中HX1是HO-或H2N-，其中[4]在甲酯皂化后作为游离酸获得。

    Antibacterial and antifungal nucleosides
    8.
    发明授权
    Antibacterial and antifungal nucleosides 失效
    抗菌和抗真菌核苷

    公开(公告)号：US5783689A

    公开(公告)日：1998-07-21

    申请号：US745732

    申请日：1996-11-12

    申请人： Marvin J. Miller ,  Julia M. Dolence ,  Manuka Ghosh

    发明人： Marvin J. Miller ,  Julia M. Dolence ,  Manuka Ghosh

    IPC分类号： C07H19/06 ,  C07H19/067

    CPC分类号： C07H19/06

    摘要： 5'-O-Acyl-5-fluorouridines and 5'-O-acyl-5-sluorocytidines are prepared by the direct acylation of the 5'-hydroxyl group with amino acids under Mitsunobu conditions and the amino acyl derivatives are coupled with other amino acids or peptides to provide antibacterial and antifungal derivatives of the nucleosides. For example, 5-fluorouridine is acylated at the 5'-hydroxyl group with an amino protected L-valine and the acylation product is deprotected to provide 5'-O-(L-valinyl)-5-fluorouridine having activity against Gram-positive bacteria including resistant staphylococcus. Preferred peptide derivatives comprise the tripeptides of ornithine and lysine wherein the terminal amino group is substituted by both hydroxy and acetyl. The latter peptides inhibit the growth of C. albicans.

    摘要翻译： 通过在Mitsunobu条件下用氨基酸直接酰化5'-羟基并将氨基酰基衍生物与其它氨基偶联，制备5'-O-酰基-5-氟尿嘧啶和5'-O-酰基-5-氟胞嘧啶 酸或肽，以提供核苷的抗细菌和抗真菌衍生物。 例如，5-氟尿苷在5'-羟基处被氨基保护的L-缬氨酸酰化，酰化产物脱保护，得到具有抗革兰氏阳性的5'- O（L-缬氨酰）-5-氟尿苷 细菌包括耐药葡萄球菌。 优选的肽衍生物包括鸟氨酸和赖氨酸的三肽，其中末端氨基被羟基和乙酰基都被羟基取代。 后一种肽抑制白念珠菌的生长。

    Process for 4-halomethyl-azetidinones by cyclization of O-acylhydroxamates
    9.
    发明授权
    Process for 4-halomethyl-azetidinones by cyclization of O-acylhydroxamates 失效
    通过O-酰基羟基化合物的环化制备4-卤代甲基 - 氮杂环丁酮的方法

    公开(公告)号：US4751296A

    公开(公告)日：1988-06-14

    申请号：US893748

    申请日：1986-08-06

    申请人： Marvin J. Miller

    发明人： Marvin J. Miller

    IPC分类号： C07B61/00 ,  C07D205/08 ,  C07D205/085 ,  C07B39/00 ,  C07D403/04 ,  C07D413/04

    CPC分类号： C07D205/085 ,  C07D205/08

    摘要： A process for 4-halomethylazetidin-2-ones is provided which comprises mixing in an inert solvent a positive halogen reagent in the presence of a weak base with a .beta.,.gamma.-unsaturated O-acylhydroxamate of the formula ##STR1## wherein R is protected amino, lower alkyl or phenyl substituted lower alkyl, R.sub.2 is a substituent such as lower alkyl which may be substituted by formyl, hydroxy, halogen, etc., and R.sub.1 is alkoxy, benzyloxy, etc. When R is a protected amino group, the process provides cis-4-halomethylazetidin-2-ones, while when R is alkyl or phenylalkyl, the trans isomer is obtained. The 4-halomethylazetidinones are useful intermediates for known antibiotic compounds.

    N-Acyloxy monocyclic .beta.-lactams
    10.
    发明授权
    N-Acyloxy monocyclic .beta.-lactams 失效
    N-酰氧基单环β-内酰胺

    公开(公告)号：US4565654A

    公开(公告)日：1986-01-21

    申请号：US479375

    申请日：1983-03-28

    申请人： Marvin J. Miller

    发明人： Marvin J. Miller

    IPC分类号： C07D205/00 ,  C07D205/08 ,  C07D205/085 ,  C07D263/00 ,  C07D413/04 ,  C07D411/12

    CPC分类号： C07D205/08 ,  C07D205/085 ,  Y02P20/55

    摘要： Process for N-acyloxy or sulfooxy 2-azetidinones comprising O-acylation of a .beta.-hydroxy or .beta.-halo hydroxamic acid, and cyclizing the O-acylhydroxamate with TPP-CCl.sub.4 -TEA or with TPP-dialkylazodicarboxylate to the N-acyloxy-2-azetidinone. Solvolysis of the acyl group provides an N-hydroxy-2-azetidinone. E.g., N-Cbz-L-serine is converted to the O-acetyl hydroxamate, cyclized and solvolyzed to N-hydroxy-3-(Cbz-amino)-2-azetidinone. The N-hydroxy-2-azetidinones are useful intermediates to monocyclic .beta.-lactam antibiotics and .beta.-lactamase inhibitors.

    摘要翻译： 包括β-羟基或β-卤代异羟肟酸的O-酰化的N-酰氧基或磺氧基-2-氮杂环丁酮的方法，并将O-酰基羟肟酸酯与TPP-CCl4-TEA或与TPP-二烷基偶氮二羧酸酯环化至N-酰氧基-2 - 氮杂环丁酮。 酰基的溶剂解解提供了N-羟基-2-氮杂环丁酮。 例如，将N-Cbz-L-丝氨酸转化为O-乙酰氧基肟基，环化并溶解分解成N-羟基-3-（Cbz-氨基）-2-氮杂环丁酮。 N-羟基-2-氮杂环丁酮是单环β-内酰胺抗生素和β-内酰胺酶抑制剂的有用中间体。