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18 条记录 (耗时 0.034 秒)

    Synthesis of (S)-3-(thien-2-ylthio)butyric acid analogs
    7.
    发明授权
    Synthesis of (S)-3-(thien-2-ylthio)butyric acid analogs 失效
    （S）-3-（噻吩-2-基硫基）丁酸类似物的合成

    公开(公告)号：US4968815A

    公开(公告)日：1990-11-06

    申请号：US510805

    申请日：1990-04-16

    申请人： Thomas J. Blacklock ,  Ichiro Shinkai

    发明人： Thomas J. Blacklock ,  Ichiro Shinkai

    IPC分类号： C07D333/34 ,  C07D495/04

    CPC分类号： C07D333/34

    摘要： (S)-3-(thien-2-ylthio)butyric acid analogs are intermediates in the synthesis of the chiral (S,S)-5,6-dihydro-4-ethylamino-6-methyl-4H-thieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide and analogs thereof, topically effective carbonic anhydrase inhibitors useful in the treatment of ocular hypertension and glaucoma. They are prepared by condensation of 2-mercaptothiophene and (R)-(+)-.beta.-methyl-.beta.-propiolactone or an analog thereof.

    Process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan e
    8.
    发明授权
    Process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecan e 失效
    制备1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8,11-四氮杂环十四烷的方法

    公开(公告)号：US5612478A

    公开(公告)日：1997-03-18

    申请号：US413582

    申请日：1995-03-30

    申请人： David Xu ,  Prasad Kapa ,  Oljan Repic ,  Thomas J. Blacklock

    发明人： David Xu ,  Prasad Kapa ,  Oljan Repic ,  Thomas J. Blacklock

    IPC分类号： C07C233/00 ,  C07C233/36 ,  C07C303/00 ,  C07C311/18 ,  C07D257/02

    CPC分类号： C07C233/36 ,  C07C311/18 ,  C07D257/02

    摘要： An improved process for preparing 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-[1,4-phenylenebis-(methylene)]-bis-1,4,8,11-tetraazacyclotetradecane.

    摘要翻译： 制备1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8,11-四氮杂环十四烷的改进方法，其包括无环四胺的选择性官能化，随后二聚和水解/甲苯磺酰化至 在第一步中获得1,4-亚苯基双 - 亚甲基桥联的六碳酰基非环状前体，在第二步中环化所述前体以获得己糖基环胞二聚体，并在第三步中对所述环化二聚体进行脱甲苯基化，然后碱化得到 所需的1,1' - [1,4-亚苯基双（亚甲基）] - 双-1,4,8,11-四氮杂环十四烷。

    Chiral catalysts for reduction of ketones and process for their preparation
    9.
    发明授权
    Chiral catalysts for reduction of ketones and process for their preparation 失效
    用于还原酮的手性催化剂及其制备方法

    公开(公告)号：US5264585A

    公开(公告)日：1993-11-23

    申请号：US966658

    申请日：1992-10-26

    申请人： Thomas J. Blacklock ,  Todd K. Jones ,  David J. Mathre ,  Lyndon C. Xavier

    发明人： Thomas J. Blacklock ,  Todd K. Jones ,  David J. Mathre ,  Lyndon C. Xavier

    IPC分类号： C07D207/08 ,  C07D495/04 ,  C07F5/02 ,  C07B41/00 ,  C07B49/00 ,  C07D211/22

    CPC分类号： C07D207/08 ,  C07D495/04 ,  C07F5/025

    摘要： The chiral catalyst of general structure 1, or its enantiomer ##STR1## is prepared by treating the corresponding N-carboxy anhydride of structure 2 ##STR2## with an aryl metal, especially a phenyl metal such as an aryl magnesium halide, aryl lithium, aryl zinc or aryl cesium, to form a 1,1-diaryl- methanol of structure 3 ##STR3## followed by treatment with a compound of structure, 4 ##STR4## The catalyst, wherein R is aromatic, is novel and in some cases superior to the catalyst wherein R is alkyl or aralkyl in directing the chirality of diborane, borane-dimethyl sulfide or borane-tetrahydrofuran reductions of ketones to secondary alcohols.

    摘要翻译： 一般结构1或其对映异构体1的手性催化剂通过用芳基金属，特别是苯基金属如芳基卤化镁，芳基锂处理结构2的相应N-羧酸酐来制备 ，芳基锌或芳基铯，以形成结构3的1,1-二芳基 - 甲醇3，然后用结构化合物4处理。其中R是芳族的催化剂是新颖的，并且在 一些情况优于催化剂，其中R是烷基或芳烷基，用于指导乙硼烷，硼烷 - 二甲基硫醚或甲硼烷 - 四氢呋喃减少酮对仲醇的手性。

    Process for racemizing an enantiomer of 5,6-dihydro-4-alkylamino-4H-thieno(or furo) [2,3-B]-thiopyran-2-sulfonamide-7,7-dioxide
    10.
    发明授权
    Process for racemizing an enantiomer of 5,6-dihydro-4-alkylamino-4H-thieno(or furo) [2,3-B]-thiopyran-2-sulfonamide-7,7-dioxide 失效
    外消旋化5,6-二氢-4-烷基氨基-4H-噻吩并[2,3-b] - 噻喃-2-磺酰胺-7,7-二氧化物的对映体的方法

    公开(公告)号：US5011942A

    公开(公告)日：1991-04-30

    申请号：US474868

    申请日：1990-02-05

    申请人： Thomas J. Blacklock ,  Edward J. J. Grabowski ,  Paul Sohar

    发明人： Thomas J. Blacklock ,  Edward J. J. Grabowski ,  Paul Sohar

    IPC分类号： C07D495/04

    CPC分类号： C07D495/04

    摘要： Compounds classified as 5,6-dihydro-4-alkylamino-4H-thieno (or furo) [2,3-b]thiopyran-2-sulfonamide-7,7-dioxide are carbonic anhydrase inhibitors useful in the treatment of ocular hypertension, and most of the carbonic anhydrase inhibitory activity resides in only one of the enantiomers. The undesired enantiomer is utilized by racemization by thermolysis of an N-acyl derivative in a basic environment followed by removal of the acyl group. The racemate may then be resolved into the enantiomers.

    摘要翻译： 分类为5,6-二氢-4-烷基氨基-4H-噻吩并（或呋喃）[2,3-b]噻喃-2-磺酰胺-7,7-二氧化物的化合物是可用于治疗高眼压症的碳酸酐酶抑制剂， 并且大多数碳酸酐酶抑制活性仅驻留在一种对映异构体中。 通过在碱性环境中热解N-酰基衍生物，然后除去酰基，通过外消旋化来利用不需要的对映异构体。 然后将外消旋物分解成对映异构体。