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    Method of preparing 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
    1.
    发明授权
    Method of preparing 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease 失效
    制备可用于治疗血栓性和血管痉挛性疾病的7-氧杂双环庚基取代的杂环酰胺前列腺素类似物的方法

    公开(公告)号：US5347007A

    公开(公告)日：1994-09-13

    申请号：US131189

    申请日：1993-10-04

    申请人： Jagabandhu Das ,  David Kronenthal

    发明人： Jagabandhu Das ,  David Kronenthal

    IPC分类号： C07D493/08 ,  C07D213/36 ,  C07D233/60

    CPC分类号： C07D493/08

    摘要： A method is provided for preparing 7-oxabicycloheptyl substituted heterocyclic aide prostaglandin analogs which are thromboxane A.sub.2 (TXA.sub.2) receptor antagonists or combined thromboxane A.sub.2 receptor antagonists/thromboxane synthetase inhibitors useful, for example, in the treatment of thrombotic and/or vasospastic disease, wherein a vinyl bromide of the formula, for example, ##STR1## wherein m, n, R.sup.1 and R.sup.2 are as defined herein is treated with a cyclizing agent to forth the corresponding oxazole.

    摘要翻译： 提供了用于制备7-氧杂二环庚基取代的杂环助剂前列腺素类似物的方法，其为血栓素A2（TXA2）受体拮抗剂或组合的血栓烷A2受体拮抗剂/血栓烷合成酶抑制剂，其可用于例如治疗血栓形成和/或血管痉挛性疾病，其中 其中m，n，R 1和R 2如本文所定义的式的溴乙烯用环化剂处理至相应的恶唑。

    Method for preparing 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
    2.
    发明授权
    Method for preparing 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease 失效
    用于治疗血栓性和血管痉挛性疾病的7-氧杂双环庚基取代的杂环酰胺前列腺素类似物的制备方法

    公开(公告)号：US5260448A

    公开(公告)日：1993-11-09

    申请号：US900383

    申请日：1992-06-18

    申请人： Jagabandhu Das ,  David Kronenthal

    发明人： Jagabandhu Das ,  David Kronenthal

    IPC分类号： C07D493/08 ,  C07D263/32

    CPC分类号： C07D493/08

    摘要： A method is provided for preparing 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs which are thromboxane A.sub.2 (TXA.sub.2) receptor antagonists or combined thromboxane A.sub.2 receptor antagonists/thromboxane synthetase inhibitors useful, for example, in the treatment of thrombotic and/or vasospastic disease, wherein a vinyl bromide of the formula, for example, ##STR1## wherein m, n, R.sup.1 and R.sup.2 are as defined herein is treated with a cyclizing agent to form the corresponding oxazole.

    摘要翻译： 提供了用于制备7-氧杂二环庚基取代的杂环酰胺前列腺素类似物的方法，其是血栓素A2（TXA2）受体拮抗剂或联合的血栓烷A2受体拮抗剂/血栓烷合成酶抑制剂，其可用于治疗血栓形成和/或血管痉挛性疾病，其中 其中m，n，R 1和R 2如本文所定义的式的溴乙烯用环化剂处理以形成相应的恶唑。

    Intramolecular arbuzov process for the preparation of intermediates useful in the preparation of phosphorus containing HMG-COA reductase inhibitors
    4.
    发明授权
    Intramolecular arbuzov process for the preparation of intermediates useful in the preparation of phosphorus containing HMG-COA reductase inhibitors 失效
    用于制备可用于制备含磷HMG-COA还原酶抑制剂的中间体的分子内arbuzov方法

    公开(公告)号：US5274155A

    公开(公告)日：1993-12-28

    申请号：US986402

    申请日：1992-12-07

    申请人： John K. Thottathil ,  David Kronenthal

    发明人： John K. Thottathil ,  David Kronenthal

    IPC分类号： C07F9/30 ,  C07F9/572 ,  C07F9/6503 ,  C07F9/6506 ,  C07F9/6596 ,  C07F7/08 ,  C07F7/18

    CPC分类号： C07F9/6596 ,  C07F9/301 ,  C07F9/5728 ,  C07F9/65033 ,  C07F9/65062

    摘要： A process for the preparation of compounds of formula ##STR1## and pharmaceutically acceptable salts thereof; wherein X is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 O-- (where O is linked to Z); Z is a hydrophobic anchor R.sub.1 is hydrogen, alkyl, cycloalkyl or aryl; comprising the steps of:(A) reacting a compound of formula ##STR2## with a compound of formula ##STR3## or a compound of formula ##STR4## in the presence of an amine base or an alkali metal hydride in an organic solvent to form a compound having the formula ##STR5## (B) heating the compound of formula IX at a temperature of from about 100.degree. C. to about 200.degree. C., to form a compound of formula ##STR6## and (C) quenching the compounds of formula VIII with an acid provides the compounds of formula I.

    摘要翻译： 制备式I化合物及其药学上可接受的盐的方法; 其中X是-CH 2 - ， - CH 2 CH 2 - ， - CH 2 CH 2 CH 2 - ， - CH = CH - ， - C 3BOND C或-CH 2 O-（其中O连接到Z）; Z是疏水锚，R1是氢，烷基，环烷基或芳基; 包括以下步骤：（A）使式II化合物与式VII化合物或式VI的化合物在胺碱或碱金属氢化物的存在下在有机物中反应 溶剂以形成具有式（VII）的化合物（B）在约100℃至约200℃的温度下加热式IX的化合物，以形成式VIII的化合物和（ C）用酸淬灭式VIII化合物，得到式Ⅰ化合物。

    (Exo,exo)-7-oxabicyclo[2.2.1]heptane-2,3-dimethanol; monoacyl ester and diacyl ester
    5.
    发明授权
    (Exo,exo)-7-oxabicyclo[2.2.1]heptane-2,3-dimethanol; monoacyl ester and diacyl ester 失效
    （Exo，外）-7-氧杂双环[2.2.1]庚烷-2,3-二甲醇; 单酰基酯和二酰基酯

    公开(公告)号：US5266710A

    公开(公告)日：1993-11-30

    申请号：US737616

    申请日：1991-07-30

    申请人： Ramesh N. Patel ,  Laszlo J. Szarka ,  John K. Thottathil ,  David Kronenthal

    发明人： Ramesh N. Patel ,  Laszlo J. Szarka ,  John K. Thottathil ,  David Kronenthal

    IPC分类号： C07D493/08 ,  C07D493/18 ,  C12P17/18 ,  C12P41/00 ,  C07D307/93

    CPC分类号： C07D493/08 ,  C12P17/181 ,  C12P41/004

    摘要： Disclosed herein is a process for preparing a novel monoester of the formula ##STR1## in which the associated novel diester ##STR2## is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the --O--C(O)--R.sup.1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]amino]methyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using this enzymatic/microbial process.

    摘要翻译： 本文公开了一种制备式“IMAGE”的新单酯的方法，其中在一种或多种能够选择性水解-OC（O））的水溶性酶或微生物的存在下水解相关新的二酯， -R1基团，其中所述处理在包含具有所述酶或微生物的水相和在所述二酯的水中不混溶的有机相的双相溶剂系统中进行。 还公开了制备[1S- [1α，2α（Z），3α，4α]] -7 - [[[[[[（1-氧代庚基）氨基]乙酰基]氨基]甲基-7 - 氧杂双环 - [2.2.1]庚-2-基] -5-庚烯酸。

    Microbiological hydrolysis for the preparation of (exo,exo)-7-oxabicyclo(2.2.1) heptane-2,3, monoacyl ester dimethanol
    6.
    发明授权
    Microbiological hydrolysis for the preparation of (exo,exo)-7-oxabicyclo(2.2.1) heptane-2,3, monoacyl ester dimethanol 失效
    用于制备（外，外）-7-氧杂双环（2.2.1）庚烷-2,3，单酰基酯二甲醇的微生物水解

    公开(公告)号：US5084387A

    公开(公告)日：1992-01-28

    申请号：US629780

    申请日：1990-12-18

    申请人： Ramesh N. Patel ,  Laszlo J. Szarka ,  John K. Thottathil ,  David Kronenthal

    发明人： Ramesh N. Patel ,  Laszlo J. Szarka ,  John K. Thottathil ,  David Kronenthal

    IPC分类号： C07D493/08 ,  C07D493/18 ,  C12P17/18 ,  C12P41/00

    CPC分类号： C07D493/08 ,  C12P17/181 ,  C12P41/004 ,  Y10S435/874

    摘要： Disclosed herein is a process for preparing a novel monoester of the formula ##STR1## in which the associated novel diester ##STR2## is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the --O--C(O)--R.sup.1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]-amino]methyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using this enzymatic/microbial process.

    摘要翻译： 本文公开了一种制备式“IMAGE”的新单酯的方法，其中在一种或多种能够选择性水解-OC（O））的水溶性酶或微生物的存在下水解相关新的二酯， -R1基团，其中所述处理在包含具有所述酶或微生物的水相和在所述二酯的水中不混溶的有机相的双相溶剂系统中进行。 还公开了制备[1S- [1α，2α（Z），3α，4α]] - [[[[[[（1-氧代庚基）氨基]乙酰基] 7-氧杂双环 - [2.2.1]庚-2-基] -5-庚烯酸。

    Process for preparing (3R-(3a.alpha.,4.beta.,7.beta..beta.,7a.alpha.))-octahydro-4,7 epoxyisobenzofuranol from associated aldehydes
    10.
    发明授权
    Process for preparing (3R-(3a.alpha.,4.beta.,7.beta..beta.,7a.alpha.))-octahydro-4,7 epoxyisobenzofuranol from associated aldehydes 失效
    从相关醛制备（3R-（3aα，4β，7ββ，7aα）） - 八氢-4,7环氧异苯并呋喃的方法

    公开(公告)号：US5084581A

    公开(公告)日：1992-01-28

    申请号：US629762

    申请日：1990-12-18

    申请人： David Kronenthal ,  John K. Thottathil

    发明人： David Kronenthal ,  John K. Thottathil

    IPC分类号： C07D493/08 ,  C07D493/18

    CPC分类号： C07D493/08

    摘要： Disclosed herein is a novel process in which novel aldehydes ##STR1## and the trans isomer thereof are hydrolyzed by treatment with an alkali metal carbonate, bicarbonate or hydroxide and water to form the cis enantiomer ##STR2## Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z), 3.alpha., 4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]-amino ]methyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using the above process.

    摘要翻译： 本文公开了一种新的方法，其中新的醛类及其反式异构体通过用碱金属碳酸盐，碳酸氢盐或氢氧化物和水进行处理而水解以形成顺式对映异构体。还公开了制备[1S - [1α，2α（Z），3α，α] -7- [3 - [[[[（1-氧代庚基）氨基]乙酰基] - 氨基]甲基-7-氧杂双环[2.2.1] 庚-2-基] -5-庚烯酸。