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1. 发明授权

US5965747A Crystalline forms of antibiotic side chain intermediates 失效
标题翻译：抗生素侧链中间体的结晶形式
公开(公告)号：US5965747A
公开(公告)日：1999-10-12
申请号：US102449
申请日：1998-06-22
申请人： Karel M. J. Brands , Ronald B. Jobson
发明人： Karel M. J. Brands , Ronald B. Jobson
IPC分类号： C07D207/16 , C07D207/08 , C07D207/12
CPC分类号： C07D207/16
摘要： Crystalline 2S-cis-3-[[(4-mercapto-2-pyrrolidinyl) carbonyl]-amino]benzoic acid and salts and solvates thereof are disclosed. Three different crystalline types are described.
摘要翻译：公开了结晶2S-顺-3 - [[（4-巯基-2-吡咯烷基）羰基] - 氨基]苯甲酸及其盐和溶剂合物。描述了三种不同的晶体类型。

2. 发明授权

US6063931A Process for synthesizing carbapenem side chain intermediates 失效
标题翻译：合成碳青霉烯侧链中间体的方法
公开(公告)号：US6063931A
公开(公告)日：2000-05-16
申请号：US106297
申请日：1998-06-29
申请人： Karel M. J. Brands , John M. Williams , Ulf H. Dolling , Ronald B. Jobson , Antony J. Davies , Ian F. Cottrell , Mark Cameron , Michael S. Ashwood
发明人： Karel M. J. Brands , John M. Williams , Ulf H. Dolling , Ronald B. Jobson , Antony J. Davies , Ian F. Cottrell , Mark Cameron , Michael S. Ashwood
IPC分类号： C07D207/16 , C07D409/12 , C07D495/08 , C07F9/572 , C07F9/32
CPC分类号： C07D409/12 , C07D207/16 , C07D495/08 , C07F9/5721 , C07F9/5722
摘要： A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.
摘要翻译：描述了合成式1化合物的方法。式2的化合物与二苯基次氯化氯反应以活化羧酸基团，然后与甲磺酰氯反应生成式4的化合物：然后使化合物4与第II族金属硫化物源在水中反应，产生式1的化合物。

3. 发明授权

US06060607A Process for synthesizing carbapenem side chain intermediates 失效
公开(公告)号：US06060607A
公开(公告)日：2000-05-09
申请号：US334398
申请日：1999-06-16
申请人： Karel M. J. Brands , John M. Williams , Ulf H. Dolling , Ronald B. Jobson , Antony J. Davies , Ian F. Cottrell , Mark Cameron , Michael S. Ashwood
发明人： Karel M. J. Brands , John M. Williams , Ulf H. Dolling , Ronald B. Jobson , Antony J. Davies , Ian F. Cottrell , Mark Cameron , Michael S. Ashwood
IPC分类号： C07D207/16 , C07D409/12 , C07F9/572 , C07D207/10
CPC分类号： C07D409/12 , C07D207/16 , C07F9/5721 , C07F9/5722
摘要： A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.

4. 发明授权

US06180783B2 Stabilized carbapenem intermediates and improved process for carbapenem synthesis 失效
标题翻译：稳定的碳青霉烯中间体和碳青霉烯合成的改进方法
公开(公告)号：US06180783B2
公开(公告)日：2001-01-30
申请号：US09093813
申请日：1998-06-09
申请人： John M. Williams , Renato T. Skerlj , Karel M. J. Brands , Ulf H. Dolling , Ronald B. Jobson
发明人： John M. Williams , Renato T. Skerlj , Karel M. J. Brands , Ulf H. Dolling , Ronald B. Jobson
IPC分类号： C07D47720
CPC分类号： C07D477/20 , Y02P20/55
摘要： A stabilized carbapenem intermediate compound represented by the formula 1: or a salt thereof is disclosed, wherein P represents a carboxyl protecting group and X represents a charge balancing group. In addition, a process for synthesizing a compound represented by formula 2: is disclosed wherein X+ is a charge balancing group, comprising: deprotecting a compound of the formula 1 to produce a compound 2.
摘要翻译：公开了由式1表示的稳定化的碳青霉烯中间体化合物或其盐，其中P表示羧基保护基，X表示电荷平衡基团。另外，公开了由式2表示的化合物的合成方法：其中 X +是电荷平衡基团，包括：使式1的化合物去保护以产生化合物2。

5. 发明授权

US4922007A Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof 失效
标题翻译： 4-氨基-1-羟基亚丁基-1,1-二膦酸或其盐的制备方法
公开(公告)号：US4922007A
公开(公告)日：1990-05-01
申请号：US363820
申请日：1989-06-09
申请人： Gerard R. Kieczykowski , David G. Melillo , Ronald B. Jobson
发明人： Gerard R. Kieczykowski , David G. Melillo , Ronald B. Jobson
IPC分类号： A61K31/66 , A61P3/00 , C07F9/38
CPC分类号： C07F9/3873
摘要： A process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-bisphosphonic acid or salts thereof which comprises:(a) reacting 4-aminobutyric acid with a mixture of phosphorous acid and PC1.sub.3 in the presence of methanesulfonic acid; and(b) recovering said 4-amino-1-hydroxybutylidene-1, 1-bisphosphonic acid or salts thereof.

6. 发明授权

US3992459A Preparation of biphenyl compounds 失效
标题翻译：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。

7. 发明授权

US4329469A Displacement purification of salts 失效
标题翻译：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。

8. 发明授权

US5872250A Process for synthesizing carbapenem antibiotics 失效
标题翻译：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。

9. 发明授权

US4220775A Preparation of 4-aza-17-substituted-5.alpha.-androstan-3-ones useful as 5.alpha.-reductase inhibitors 失效
标题翻译：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;

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