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    Method for producing D-.alpha.-amino acid
    1.
    发明授权
    Method for producing D-.alpha.-amino acid 失效
    D-α-氨基酸的制备方法

    公开(公告)号：US4211840A

    公开(公告)日：1980-07-08

    申请号：US897003

    申请日：1978-04-17

    申请人： Shigeru Nakamori ,  Kenzo Yokozeki ,  Koji Mitsugi ,  Chikahiko Eguchi ,  Hisao Iwagami

    发明人： Shigeru Nakamori ,  Kenzo Yokozeki ,  Koji Mitsugi ,  Chikahiko Eguchi ,  Hisao Iwagami

    IPC分类号： C07D233/72 ,  C12P13/04 ,  C12P13/24

    CPC分类号： C12P13/04

    摘要： D-.alpha.-amino acids are produced by contacting a 5-substituted hydantoin with an effective amount of an enzyme capable of converting the 5-substituted hydantoin to the D-.alpha.-amino acid produced by a microorganism in an aqueous medium at a pH in the range of 4 to 9, the microorganism being capable of utilizing the D-isomer of the 5-substituted hydantoin as the sole nitrogen source, but substantially incapable of utilizing the L-isomer of the 5-substituted hydantoin as the nitrogen source and the substituent of the 5-position being such that upon reaction with the enzyme, an optically active D-.alpha.-amino acid isomer is produced; and recovering the D-.alpha.-amino acid which accumulates in the aqueous medium.

    摘要翻译： D-α-氨基酸是通过使5-取代的乙内酰脲与有效量的能够将5-取代的乙内酰脲转化为由微生物在水性介质中产生的D-α-氨基酸的酶在pH值 范围为4至9，微生物能够利用5-取代乙内酰脲的D-异构体作为唯一的氮源，但基本上不能利用5-取代的乙内酰脲的L-异构体作为氮源， 5位的取代基使得当与酶反应时，产生光学活性的D-α-氨基酸异构体; 并回收积聚在水性介质中的D-α-氨基酸。

    Process for preparing 2',3'-dideoxyadenosine
    2.
    发明授权
    Process for preparing 2',3'-dideoxyadenosine 失效
    制备2'，3'-二脱氧腺苷的方法

    公开(公告)号：US5290927A

    公开(公告)日：1994-03-01

    申请号：US317567

    申请日：1989-03-01

    申请人： Yutaka Honda ,  Hiroshi Shiragami ,  Hisao Iwagami ,  Masayuki Arai

    发明人： Yutaka Honda ,  Hiroshi Shiragami ,  Hisao Iwagami ,  Masayuki Arai

    IPC分类号： C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H19/173 ,  C07H19/073

    CPC分类号： C07H19/04 ,  C07H19/06 ,  C07H19/16

    摘要： A process for preparing 2',3'-dideoxyadenosine of the formula ##STR1## wherein B is adenine, wherein R.sup.1 is hydrogen, C.sub.1-12 acyl, C.sub.1-12 alkyl, C.sub.7-8 aralkyl, or silyl, said process comprising:reducing a nucleoside of the formula IIIa or IIIb ##STR2## wherein R.sup.2 is hydrogen, C.sub.1-12 acyl, C.sub.1-12 alkyl, C.sub.7-8 aralkyl or silyl; X is Cl, Br or I; R.sup.5 is C.sub.1-12 acyl and B is adenine, with hydrogen in the presence of a palladium catalyst and aqueous solvent mixture of acetonitrile or ethyl acetate and water, said aqueous solvent containing a base selected from the group consisting of sodium hydroxide/sodium acetate and sodium carbonate/sodium acetate, wherein said solvent has a pH of 9-11.

    摘要翻译： 一种制备式“IMAGE”的2'，3'-二脱氧腺苷的方法，其中B是腺嘌呤，其中R 1是氢，C 1-12酰基，C 1-12烷基，C 7-8芳烷基或甲硅烷基，所述方法包括： （IIIa）（IIIb）其中R2是氢，C1-12酰基，C1-12烷基，C7-8芳烷基或甲硅烷基的式IIIa或IIIb的核苷。 X是Cl，Br或I; R5是C1-12酰基，B是腺嘌呤，在钯催化剂和乙腈或乙酸乙酯与水的水溶剂混合物的存在下，氢气，所述含水溶剂含有选自氢氧化钠/乙酸钠和 碳酸钠/乙酸钠，其中所述溶剂的pH为9-11。

    4-Methylsulfonyl-azetidinone derivatives
    4.
    发明授权
    4-Methylsulfonyl-azetidinone derivatives 失效
    4-甲基磺酰基 - 氮杂环丁酮衍生物

    公开(公告)号：US4537719A

    公开(公告)日：1985-08-27

    申请号：US431557

    申请日：1982-09-30

    申请人： Toshihisa Kato ,  Hisao Iwagami ,  Naohiko Yasuda

    发明人： Toshihisa Kato ,  Hisao Iwagami ,  Naohiko Yasuda

    IPC分类号： C07D205/08 ,  A61K31/395 ,  A61K31/397 ,  A61P31/04 ,  C07D205/09 ,  C07D205/095 ,  C07D403/12 ,  A61K31/495

    CPC分类号： C07D403/12 ,  C07D205/09 ,  C07D205/095

    摘要： The present invention relates to novel azetidinone derivatives of the general formula: ##STR1## where n is 0 or 2,X is hydrogen, halogen, amino, alkylamino, benzylamino or acylamino, andY is ##STR2## R is lower alkyl, 2,2,2-trichloroethyl, or aralkyl; and M is hydrogen or alkali metal having .beta.-lactamase inhibiting activity.The derivatives of the present invention can be administered together with antibiotics having a .beta.-lactam ring as antibacterial agents against .beta.-lactamase producing bacteria.A method for synthesizing said azetidinone derivatives is also disclosed.

    摘要翻译： 本发明涉及以下通式的新的氮杂环丁酮衍生物：其中n为0或2，X为氢，卤素，氨基，烷基氨基，苄基氨基或酰基氨基，Y为低级烷基， 2,2-三氯乙基或芳烷基; M是具有β-内酰胺酶抑制活性的氢或碱金属。 本发明的衍生物可以与具有β-内酰胺环的抗生素一起作为产生β-内酰胺酶的细菌的抗菌剂一起施用。 还公开了合成所述氮杂环丁酮衍生物的方法。

    5-Substituted-3-isoxazolecarboxylic acid derivatives
    5.
    发明授权
    5-Substituted-3-isoxazolecarboxylic acid derivatives 失效
    5-取代的3-异恶唑羧酸衍生物

    公开(公告)号：US4465631A

    公开(公告)日：1984-08-14

    申请号：US482544

    申请日：1983-04-06

    申请人： Naohiko Yasuda ,  Hisao Iwagami ,  Eiji Nakanishi ,  Yukio Sasaki ,  Shigeru Yamanaka

    发明人： Naohiko Yasuda ,  Hisao Iwagami ,  Eiji Nakanishi ,  Yukio Sasaki ,  Shigeru Yamanaka

    IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D499/00 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D501/20 ,  C07D501/22 ,  C07D501/44

    CPC分类号： C07D499/00

    摘要： A 5-substituted-3-isoxazolecarboxylic acid derivative of the general formula: ##STR1## wherein X stands for a phenyl group, thienyl group, furyl group or pyridyl group, each of which optionally may carry at least one substituent group; R stands for a phenyl group or hydroxyphenyl group; and A stands for a group of the formula: ##STR2## wherein Y stands for ##STR3## in which the carbon atom with which the carboxyl group combines with the nitrogen atom in A, M stands for a hydrogen atom or a substituent group, and Z stands for a hydrogen atom, hydroxy group, acyloxy group, carbamoyloxy group, aromatic heterocycle thio group or aromatic nitrogen-containing heterocycle quaternary ammonium group, is disclosed along with methods for producing these compounds.

    摘要翻译： 其中X代表苯基，噻吩基，呋喃基或吡啶基，其中每一个可以任选地带有至少一个取代基;一个5-取代的3-异恶唑羧酸衍生物，其通式如下： R代表苯基或羟基苯基; A代表下式的基团：其中Y代表其中羧基与A中的氮原子结合的碳原子，M代表氢原子或取代基的，以及 Z表示氢原子，羟基，酰氧基，氨基甲酰氧基，芳香族杂环硫基或芳香族含氮杂环季铵基，同时也包括这些化合物的制造方法。

    Process for preparing 2', 3'- dideoxyinosine
    7.
    发明授权
    Process for preparing 2', 3'- dideoxyinosine 失效
    制备2'，3'-二脱氧肌苷的方法

    公开(公告)号：US5466793A

    公开(公告)日：1995-11-14

    申请号：US860605

    申请日：1992-03-30

    申请人： Yutaka Honda ,  Hiroshi Shiragami ,  Hisao Iwagami ,  Masayuki Arai

    发明人： Yutaka Honda ,  Hiroshi Shiragami ,  Hisao Iwagami ,  Masayuki Arai

    IPC分类号： C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H19/173 ,  C07H19/073

    CPC分类号： C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  Y02P20/55

    摘要： A process for preparing 2',3'-dideoxyinosine comprising reducing a nucleoside of the formula IIIa or IIIb ##STR1## wherein R.sup.2 is hydrogen, C.sub.1-12 acyl, C.sub.1-12 alkyl, C.sub.7-8 aralkyl or a silyl protecting group; X is Cl, Br, or I; R.sub.5 is C.sub.1-12 acyl; H.sub.x is hypoxanthine; with hydrogen in the presence of a palladium catalyst; wherein said reduction is conducted in a solvent containing a base of pH 9-11 and wherein the solvent is acetonitrile, aqueous acetonitrile, aqueous ethyl acetate, or aqueous methanol.

    摘要翻译： 制备2'，3'-二脱氧肌苷的方法，包括还原式IIIa或IIIb的核苷（IIIa）（IIIb）其中R2是氢，C1-12酰基，C1-12烷基，C7- 8芳烷基或甲硅烷基保护基; X是Cl，Br或I; R5是C1-12酰基; Hx是次黄嘌呤; 在钯催化剂存在下用氢气; 其中所述还原在含有pH9-11的碱的溶剂中进行，其中溶剂是乙腈，乙腈水溶液，乙酸乙酯水溶液或甲醇水溶液。

    Method of preparing sodium salts of imidazoledicarboxylic acid substituted cephalosporin derivatives
    9.
    发明授权
    Method of preparing sodium salts of imidazoledicarboxylic acid substituted cephalosporin derivatives 失效
    制备咪唑二羧酸取代头孢菌素衍生物的钠盐的方法

    公开(公告)号：US4423215A

    公开(公告)日：1983-12-27

    申请号：US353809

    申请日：1982-03-02

    申请人： Naohiko Yasuda ,  Hisao Iwagami ,  Yasuo Irie ,  Eiji Nakanishi ,  Hideomi Saito

    发明人： Naohiko Yasuda ,  Hisao Iwagami ,  Yasuo Irie ,  Eiji Nakanishi ,  Hideomi Saito

    IPC分类号： C07D501/04 ,  C07D501/38 ,  C07D501/46

    CPC分类号： C07D501/46

    摘要： A method of preparing sodium salts of an imidazoledicarboxylic acid derivative of a substituted cephalosporin represented by the general formula of ##STR1## where X is a radical selected from the group consisting of hydrogen, halogen, hydroxyl, alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, alkylsulfinyl, arylsulfinyl, aralkylsulfinyl, amino, mono- or dialkylamino, mono- or diarylamino, mono- or diaralkylamino, acylamino, sulfonic acid, nitro or heterocyclic group;and where R is a radical selected from hydrogen, an organic radical such as alkyl, aryl or aralkyl or a heterocyclic group, said organic radical and heterocyclic group being optionally substituted;said method comprising reacting a compound represented by the following formula: ##STR2## with 4-pyridineethanesulfonic acid in an aqueous solution of sodium iodide and subsequently recovering the salt.The compounds are useful in the treatment of bacterial infections, particularly Pseudomonas aeruginosa, in man and other animals.

    摘要翻译： 一种制备由通式（I）＆lt; IMAGE＆gt;表示的取代头孢菌素的咪唑二羧酸衍生物的钠盐的方法，其中X是选自氢，卤素，羟基，烷基，芳基 芳烷氧基，烷氧基，芳氧基，芳烷硫基，芳烷硫基，烷基磺酰基，芳基磺酰基，芳烷基磺酰基，烷基亚磺酰基，芳基亚磺酰基，芳烷基亚磺酰基，氨基，一烷基氨基或二芳基氨基，单或二芳基氨基， ，硝基或杂环基; 并且其中R是选自氢，有机基团如烷基，芳基或芳烷基或杂环基的基团，所述有机基团和杂环基团任选被取代; 所述方法包括将由下式表示的化合物与4-吡啶乙磺酸在碘化钠水溶液中反应，随后回收盐。 这些化合物可用于治疗人和其他动物中细菌感染，特别是铜绿假单胞菌（Pseudomonas aeruginosa）。