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9 条记录 (耗时 0.034 秒)

    Process for synthesizing carbapenem antibiotics
    5.
    发明授权
    Process for synthesizing carbapenem antibiotics 失效
    合成碳青霉烯类抗生素的方法

    公开(公告)号：US5872250A

    公开(公告)日：1999-02-16

    申请号：US887849

    申请日：1997-07-30

    申请人： John M. Williams ,  Ronald B. Jobson

    发明人： John M. Williams ,  Ronald B. Jobson

    IPC分类号： C07D477/02 ,  C07D477/20 ,  C07D207/16

    CPC分类号： C07D477/20 ,  C07D477/02 ,  Y02P20/55

    摘要： A process for synthesizing a compound of the formula I: ##STR1## or a pharmaceutically acceptable salt or ester thereof, wherein each P independently represents H or a protecting group, and R.sup.1 and R.sup.2 independently represent H, C.sub.1-10 alkyl, aryl or heteroaryl, or substituted C.sub.1-10 alkyl, aryl or heteroaryl, comprising:reacting the compounds: ##STR2## or a pharmaceutically acceptable salt or ester thereof, and ##STR3## or a pharmaceutically acceptable salt or ester thereof, wherein X represents OP(O)(OR).sub.2, or OSO.sub.2 R, wherein R represents C.sub.1-6 alkyl, aryl or perfluoro C.sub.1-6 alkyl, in the presence of an amine selected from the group consisting of: diisopropylamine (DIPA), dicyclohexylamine (DCHA), 2,2,6,6-tetramethylpiperidine (TMP), 1,1,3,3-tetramethylguanidine (TMG), 1,8-diazabicyclo�4.3.0!undec-7-ene (DBU) and 1,5-diazabicyclo�4.3.0!non-5-ene to produce a compound of formula I.

    摘要翻译： 合成式I化合物或其药学上可接受的盐或酯的方法，其中每个P独立地表示H或保护基，并且R 1和R 2独立地表示H，C 1-10烷基，芳基或 杂芳基或取代的C 1-10烷基，芳基或杂芳基，其包括：使化合物：II或其药学上可接受的盐或酯，和其药学上可接受的盐或酯，其中X表示OP （O）（OR）2或OSO 2 R，其中R表示C 1-6烷基，芳基或全氟C 1-6烷基，在选自二异丙胺（DIPA），二环己胺（DCHA）， 2,2,6,6-四甲基哌啶（TMP），1,1,3,3-四甲基胍（TMG），1,8-二氮杂双环[4.3.0]十一碳-7-烯（DBU）和1,5-二氮杂双环 [4.3.0]壬-5-烯，以制备式I化合物。

    Preparation of biphenyl compounds
    7.
    发明授权
    Preparation of biphenyl compounds 失效
    联苯化合物的制备

    公开(公告)号：US3992459A

    公开(公告)日：1976-11-16

    申请号：US571165

    申请日：1975-05-01

    申请人： Torleif Utne ,  Ronald B. Jobson ,  Alfred V. Lovell

    发明人： Torleif Utne ,  Ronald B. Jobson ,  Alfred V. Lovell

    IPC分类号： C07C51/15 ,  C07C25/18

    CPC分类号： C07C51/15

    摘要： Biaryl coupling, particularly to form 2,4-difluorobiphenyl, is accomplished by diazotizing an aniline and coupling the benzenediazonium salt with a second aromatic component in the presence of a strong acid, an inert finely divided solid and copper powder or a copper salt.

    摘要翻译： 特别是用于形成2,4-二氟联苯的双芳基偶合是通过在强酸，惰性细分固体和铜粉或铜盐存在下，使苯胺重氮化和偶联苯二胺盐与第二芳族组分来实现的。

    Displacement purification of salts
    8.
    发明授权
    Displacement purification of salts 失效
    盐的位移纯化

    公开(公告)号：US4329469A

    公开(公告)日：1982-05-11

    申请号：US209814

    申请日：1980-11-24

    申请人： Torleif Utne ,  Ronald B. Jobson

    发明人： Torleif Utne ,  Ronald B. Jobson

    IPC分类号： C07D211/70

    CPC分类号： C07D211/70

    摘要： An optically impure diastereomeric salt is purified by treating a suspension of the salt in an appropriate solvent or solvent mixture with the required amount of the desired, optically pure, acid or base.

    摘要翻译： 通过在合适的溶剂或溶剂混合物中用所需量的所需光学纯的酸或碱处理盐的悬浮液来纯化光学上不纯的非对映体盐。

    Preparation of 4-aza-17-substituted-5.alpha.-androstan-3-ones useful as 5.alpha.-reductase inhibitors
    9.
    发明授权
    Preparation of 4-aza-17-substituted-5.alpha.-androstan-3-ones useful as 5.alpha.-reductase inhibitors 失效
    可用作5α-还原酶抑制剂的4-氮杂-17-取代-5α-雄甾烷-3-酮的制备

    公开(公告)号：US4220775A

    公开(公告)日：1980-09-02

    申请号：US20372

    申请日：1979-03-15

    申请人： Gary H. Rasmusson ,  David B. R. Johnston ,  Donald F. Reinhold ,  Torleif Utne ,  Ronald B. Jobson

    发明人： Gary H. Rasmusson ,  David B. R. Johnston ,  Donald F. Reinhold ,  Torleif Utne ,  Ronald B. Jobson

    IPC分类号： C07C62/24 ,  C07J1/00 ,  C07J3/00 ,  C07J21/00 ,  C07J33/00 ,  C07J41/00 ,  C07J43/00 ,  C07J73/00 ,  C07D221/18

    CPC分类号： C07J43/003 ,  C07C62/24 ,  C07J1/0022 ,  C07J21/00 ,  C07J3/005 ,  C07J33/007 ,  C07J41/0016 ,  C07J41/0066 ,  C07J73/005 ,  C07C2103/16 ,  Y10S514/859

    摘要： A method of preparing a compound of the formula: ##STR1## where Formula (I) may also have the structure of partial Formula (III); wherein, ##STR2## R' is hydrogen or methyl; R" is hydrogen or .beta.-methyl;R'" is .beta.-methyl or hydroxy;Z is (1) oxo;(2) .beta.-hydrogen and .alpha.-hydroxy; or .alpha.-hydrogen or .alpha.-hydroxyl and(3) (Y).sub.n Q where n=0 or 1, Y is a straight or branched hydrocarbon chain of 1 to 12 carbon atoms andQ is ##STR3## where R.sup.8 is, ##STR4## where the dashed bond replaces the 17.alpha. hydrogen; (6) cyano; or(7) tetrazolyl;and pharmaceutically acceptable salts of the above compounds;CHARACTERIZED IN THAT(I.) a compound of the formula: ##STR5## , where A has the meanings above except --CH.dbd.CH--, is (1) treated with an oxidizing agent at reduced temperatures to form the corresponding 5-oxo-3,5-seco-androstan-3-oic acid compound;(2) treating the product of step (1) with an amine of formula: R.sup.1 NH.sub.2 to form the corresponding 4-aza-5-androsten-3-one compound substituted in the 4-position with R.sup.1 ; and(3) treating the product of step (2) with hydrogen under catalytic conditions to form the compound of Formula I and I & II wherein B is ##STR6## (II.) and where it is desired to prepare compounds of Formula I wherein B is ##STR7## additionally carrying out the following steps on the products prepared by the procedures in (I.) above:(1) alkylating the lactim carbonyl by treating it with trialkyloxonium tetrafluoroborate to form the corresponding alkyl iminium ether, i.e., the compound of Formula I where B is as above and R.sup.4 =OR.sup.5 ;(2) treating the product of step (1) with an amine of formula HNR.sup.6 R.sup.7 followed by treatment with a mineral acid to form the compound of Formula I where B is as above and R.sup.4 =NR.sup.6 R.sup.7 ;(III.) and where it is desired to prepare compounds of Formula I wherein A is --CH.dbd.CH--, additionally carrying out the following steps on the products prepared by the procedures in (I.) above:(1) treating the 1,2 saturated compound with lithium diisopropyl amide to form the corresponding enolate;(2) treating the enolate of step (1) in situ with diphenyldisulfide to form the corresponding .alpha.-phenylthio compound;(3) oxidizing the product of step (2) to form the corresponding sulfoxide compound; and(4) heating the product of step (3) to form the compound of Formula I wherein A is --CH.dbd.CH--.

    摘要翻译： 制备下式化合物的方法：其中式（I）还可以具有部分式（III）的结构; 其中，A为（1）CH 2 CH 2; （2）CHCH; R图像是氢或甲基; R“是氢或β-甲基; R“'是β-甲基或羟基; Z是（1）氧代; （2）β-氢和α-羟基; 或（3）（Y）n Q其中n = 0或1，Y为1至12个碳原子的直链或支链烃链，Q为（a）其中R8为 （4）（5）其中虚线键代替17α氢; （6）氰基; 或（7）四唑基;