公开(公告)号：US5041660A

公开(公告)日：1991-08-20

申请号：US602391

申请日：1990-10-24

申请人： Keiichi Yokoyama ,  Yoshio Noguchi ,  Noriaki Kihara

发明人： Keiichi Yokoyama ,  Yoshio Noguchi ,  Noriaki Kihara

IPC分类号： C07C323/41 ,  C07C67/00 ,  C07C313/00 ,  C07C319/14 ,  C07C319/18 ,  C07C323/40 ,  C07C323/42 ,  C07D233/54

CPC分类号： C07D233/64

摘要： Disclosed is a novel .alpha.-chloroketone derivative as a synthesis intermediate of N-cyano-N'-methyl-N"-(2-((5-methyl-1H-imidazol-4-yl)methylthio)ethyl)guanidine (general name: Cimetidine) which shows an action of controlling the secretion of gastric acid and is valuable as a medicine for remedy of a gastric ulcer. This .alpha.-chloroketone derivative is prepared by reacting disulfide derivative with sulfuryl chloride and reacting the reaction product with methylvinyl ketone or by reacting a mercapto derivative with 3-chloro-3-buten-2-one.

公开(公告)号：US5021441A

公开(公告)日：1991-06-04

申请号：US326939

申请日：1989-03-22

申请人： Stephen R. Baker ,  Alec Todd

发明人： Stephen R. Baker ,  Alec Todd

IPC分类号： A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/275 ,  A61P37/08 ,  A61P43/00 ,  C07C319/14 ,  C07C323/44 ,  C07C323/52 ,  C07C323/56 ,  C07C323/59 ,  C07C323/60 ,  C07D257/04 ,  C07D303/08 ,  C07D405/04 ,  C07D405/10

CPC分类号： C07D257/04 ,  C07D405/04

摘要： There are disclosed pharmaceutical compounds of the formula: ##STR1## in which R.sup.1 is halo-substituted alkyl;X is alkenylene; and R.sup.1 --X-- contains 6 to 34 carbon atoms;R.sup.2 is C.sub.1-5 alkyl substituted by(i) optionally protected carboxyl, nitrile, optionally protected tetrazolyl or --CONR'R", in which R' and R" are each hydrogen or C.sub.1-4 alkyl, ##STR2## (ii) in which R' and R" are each hydrogen or C.sub.1-4 alkyl, or ##STR3## (iii) in which R', R" and R'" are each hydrogen or C.sub.1-4 alkyl, or R.sup.2 is a group of the formula ##STR4## in which R' is hydrogen or an optionally protected amino acid residue, and R" is --OH or an optionally protected amino acid residue; andR.sup.3, R.sup.4 and R.sup.5 are each hydrogen, optionally protected carboxyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro or --CONR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl; and salts thereof.

公开(公告)号：US4985180A

公开(公告)日：1991-01-15

申请号：US359981

申请日：1989-06-06

申请人： Harold E. Bellis ,  Donald J. Dumas ,  George C. Sonnichsen ,  Vinayakam Subramanyam

发明人： Harold E. Bellis ,  Donald J. Dumas ,  George C. Sonnichsen ,  Vinayakam Subramanyam

IPC分类号： B01J31/02 ,  C07B61/00 ,  C07C219/28 ,  C07C229/06 ,  C07C303/22 ,  C07C303/32 ,  C07C305/18 ,  C07C305/24 ,  C07C309/24 ,  C07C309/42 ,  C07C319/14 ,  C07C323/52 ,  C07F9/54

CPC分类号： C07C309/42 ,  C07F9/5407

摘要： Phenyl esters of substituted acids are prepared by a two-step process in which a phenol derivative is first treated with an acid halide to yield a phenyl ester intermediate, and the intermediate is reacted with an appropriate nucleophile.

摘要翻译： 取代酸的苯酯通过两步法制备，其中首先用酰卤处理苯酚衍生物，得到苯酯中间体，并使中间体与合适的亲核试剂反应。

公开(公告)号：US4968836A

公开(公告)日：1990-11-06

申请号：US472677

申请日：1990-01-30

申请人： Hans-Ruedi Kanel ,  John G. Dingwall

发明人： Hans-Ruedi Kanel ,  John G. Dingwall

IPC分类号： C07C41/18 ,  C07C43/12 ,  C07C43/192 ,  C07C43/225 ,  C07C201/12 ,  C07C205/37 ,  C07C253/30 ,  C07C255/54 ,  C07C303/22 ,  C07C303/32 ,  C07C309/08 ,  C07C319/14 ,  C07C323/22 ,  C07D307/20

CPC分类号： C07C43/12 ,  C07C303/22 ,  C07D307/20 ,  C07C2101/02

摘要： The invention relates to a process for the preparation of cyclopropanecarbaldehydes of formula ##STR1## in which R.sub.1 is C.sub.1 -C.sub.4 alkyl or benzyl, which comprises (a) reacting a tetrahydrofuran of formula ##STR2## in which X is halogen and R.sub.2 is unsubstituted or halo-substituted C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.6 -cycloalkyl that is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl or by C.sub.1 -C.sub.4 alkoxy, or phenyl or benzyl each of which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro or cyano, with a halogenating agent to form a 1,2,4-trihalobutyl ether of formula ##STR3## in which X is halogen and R.sub.2 is unsubstituted or halo-substituted C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.6 cycloalkyl that is unsubstituted or substituted by halogen C.sub.1 -C.sub.4 alkyl or by C.sub.1 -C.sub.4 alkoxy, or phenyl or benzyl each of which is unsubstituted or substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro or cyano, and(b) then reacting the compound of formula III with an aqueous bisulfite solution to form a bisulfite adduct of formula ##STR4## in which X is a halogen and Y is a cation equivalent of an alkali metal or alkaline earth metal ion, and(c) then cyclising the adduct, in the presence of a base, with a thiolate of formulaR.sub.1 --S.sup..crclbar. Z.sup..sym. (V) in which R.sub.1 is C.sub.1 -C.sub.4 alkyl or benzyl and Z is a cation equivalent of an alkali metal or alkaline earth metal ion, to form a cyclopropanecarbaldehyde of formula I, and to the individual Process Steps (a), (b) and (c) and the combinations thereof (a)+(b) and (b)+(c), and to the novel intermediates of formulae III and IV.

摘要翻译： 本发明涉及一种制备式（I）的环丙烷甲醛的方法，其中R 1是C 1 -C 4烷基或苄基，其包括（a）使式Ⅺ（II）的四氢呋喃与其中X是卤素 未取代或被卤素，C 1 -C 4烷基或C 1 -C 4烷氧基取代的C 1 -C 10烷基，C 3 -C 6环烷基，或未被取代或被卤素取代的苯基或苄基， C 1-4烷基，C 1 -C 4烷氧基，硝基或氰基，与卤化剂反应形成式（Ⅺ）的1,2,4-三卤代丁基醚，其中X为卤素，R 2为未取代的或卤素取代的C 1 -C 10烷基， C 3 -C 6环烷基，其未被取代或被卤素C 1 -C 4烷基或C 1 -C 4烷氧基取代，或苯基或苄基，其各自未被取代或被卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，硝基或氰基取代，和（b） 使式III化合物与亚硫酸氢钠水溶液反应，形成亚硫酸氢盐加合物o （IV）其中X是卤素，Y是碱金属或碱土金属离子的阳离子当量，和（c）然后在碱的存在下将加合物与硫醇的硫醇盐环化 式中R 1为C 1 -C 4烷基或苄基并且Z为碱金属或碱土金属离子的阳离子当量的式R1-S（ - ）Z（+）（V），形成式I的环丙烷甲醛， 单独的方法步骤（a），（b）和（c）及其组合（a）+（b）和（b）+（c）以及式III和IV的新型中间体。

公开(公告)号：US4966732A

公开(公告)日：1990-10-30

申请号：US73584

申请日：1987-07-15

申请人： Guenes Giray ,  Klaus Huthmacher ,  Axel Kleemann ,  Thomas Lied

发明人： Guenes Giray ,  Klaus Huthmacher ,  Axel Kleemann ,  Thomas Lied

IPC分类号： C07C323/52 ,  A61K31/385 ,  A61P1/16 ,  A61P25/00 ,  C07C67/00 ,  C07C313/00 ,  C07C319/06 ,  C07C319/14 ,  C07C319/20 ,  C07C323/22 ,  C07C327/22 ,  C07D339/04

CPC分类号： C07D339/04 ,  C07C323/00

摘要： 1,2-Dithiolane-3-pentanoic acid (D,L-thioctic acid) of the formula ##STR1## is prepared by a process comprising (a) reacting a 2-(3-alkylthiopropionyl)-cyclopentanone-1 of the formula ##STR2## where R is a C.sub.1 -C.sub.4 alkyl, phenyl or benzyl in aqueous alkaline solution at a temperature of about 20.degree. C. to about 90.degree. C. to form the corresponding carboxylic acid of formula VI ##STR3## (b) reacting the compound of formula VI with an alkyl mercaptan at a temperature between -20.degree. C. and 0.degree. C. to form the corresponding thioketal of formula VII ##STR4## (c) reacting the compound of formula VII with sodium in liquid ammonia at temperature temperture between -60.degree. C. and -10.degree. C. to form the 6,8-dimercaptooctanic acid of formual VIII ##STR5## (d) reacting the 6,8-dimercaptooctanoic acid of formula VIII in alkaline solution with an iron (III) salt and oxygen to form the 1,2-dithiolane-3-pentanoic acid of formula IX, or in place of steps (a) through (c) reacting an acid of formula XII ##STR6## where R.sub.1 and R.sub.2 are hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl or benzyl, with the proviso that both R.sub.1 and R.sub.2 cannot be benzyl, with sodium in liquid ammonia at a temperature between -60.degree. C. and -10.degree. C. to form the corresponding 6,8-dimercaptooctanoic acid of formula VIII. The compounds of formulae VI, VII, XII are new.

公开(公告)号：USRE33300E

公开(公告)日：1990-08-14

申请号：US430697

申请日：1989-11-01

申请人： Stephen R. Baker ,  William B. Jamieson ,  Alec Todd

发明人： Stephen R. Baker ,  William B. Jamieson ,  Alec Todd

IPC分类号： A61K31/165 ,  A61K31/10 ,  A61K31/135 ,  A61K31/16 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/235 ,  A61K31/275 ,  A61K31/41 ,  A61K38/00 ,  A61P11/00 ,  A61P37/08 ,  A61P43/00 ,  C07C17/26 ,  C07C17/354 ,  C07C33/20 ,  C07C33/30 ,  C07C67/00 ,  C07C313/00 ,  C07C315/02 ,  C07C317/00 ,  C07C317/14 ,  C07C317/18 ,  C07C317/28 ,  C07C317/44 ,  C07C317/46 ,  C07C317/48 ,  C07C319/14 ,  C07C323/12 ,  C07C323/16 ,  C07C323/25 ,  C07C323/52 ,  C07C323/56 ,  C07C323/58 ,  C07C323/60 ,  C07C323/65 ,  C07D257/04 ,  C07D257/06 ,  C07D303/02 ,  C07D303/04 ,  C07D303/08 ,  C07D303/12 ,  C07D303/14 ,  C07D303/32 ,  C07D303/38 ,  C07D303/40 ,  C07D303/46 ,  C07D307/88 ,  C07D309/12 ,  C07D405/10 ,  C07K5/06 ,  C07K5/062

CPC分类号： C07D257/04 ,  C07C17/2635 ,  C07C17/354 ,  C07C255/00 ,  C07C309/00 ,  C07C317/00 ,  C07C323/00 ,  C07C33/20 ,  C07C33/30 ,  C07D303/04 ,  C07D303/14 ,  C07D303/32 ,  C07D303/38 ,  C07D303/40 ,  C07D307/88 ,  C07D309/12 ,  C07D405/10 ,  C07K5/0606 ,  A61K38/00 ,  Y02P20/55

摘要： There are described compounds of formula ##STR1## in which n is 0, 1 or 2, R.sup.1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R.sup.2 is optionally substituted phenyl or C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro and --CONR.sub.2.sup.10 where each R.sup.10 is hydrogen or C.sub.1-4 alkyl; and salts thereof. The compounds are leukotriene antagonists.

公开(公告)号：US4879414A

公开(公告)日：1989-11-07

申请号：US156692

申请日：1988-02-17

申请人： Grannis S. Johnson ,  Reuben H. Grinstein ,  Stuart J. Hartman ,  Raymond P. Dallago

发明人： Grannis S. Johnson ,  Reuben H. Grinstein ,  Stuart J. Hartman ,  Raymond P. Dallago

IPC分类号： B01J23/04 ,  B01J31/02 ,  C07B61/00 ,  C07C319/02 ,  C07C319/14 ,  C07C323/25 ,  C08G59/18 ,  C08G59/40 ,  C08G59/66

CPC分类号： C07C323/25 ,  C08G59/182 ,  C08G59/66 ,  C07C2101/14

摘要： Polythiols prepared by the reaction of hydrogen sulfide or organic dithiols with polyglycidyl substituted amines have been found to be outstanding curing agents for epoxy resins. Epoxy resins cured with these polythiols are characterized by not only improved gel times, but also improved cure rates, better heat resistance and greater resistance to absorption of water.A useful polythiol is the reaction product of N,N,N',N'-tetraglycidyl-m-xylylenediamine with hydrogen sulfide.

公开(公告)号：US4845299A

公开(公告)日：1989-07-04

申请号：US177620

申请日：1988-04-05

申请人： Masami Haga

发明人： Masami Haga

IPC分类号： C07C319/14 ,  C07C67/00 ,  C07C313/00 ,  C07C319/16 ,  C07C319/22 ,  C07C323/20

CPC分类号： C07C323/00

摘要： The bis(hydroxyphenyl) sulfides mixture prepared according to the inventive method is advantageous in respect of the increased proportion of 4-mercaptophenol relative to less useful 2-mercaptophenol in the product obtained by the reductive decomposition of the mixture. The inventive method is characterized by performing the reaction of phenol and sulfur chloride in a specific solvent which is an ethylene glycol monoalkyl ether compound such as ethylene glycol monomethyl ether, triethylene glycol monoethyl ether and the like.

公开(公告)号：US4841089A

公开(公告)日：1989-06-20

申请号：US937935

申请日：1986-12-04

申请人： Hermann Hagemann ,  Klaus Sasse

发明人： Hermann Hagemann ,  Klaus Sasse

IPC分类号： C07D239/38 ,  C07C67/00 ,  C07C313/00 ,  C07C319/14 ,  C07C323/62 ,  C07D213/70

CPC分类号： C07C323/00

摘要： 4-Mercaptobenzonitriles are prepared by reacting the appropriate 4-halogenobenzonitrile with sodium sulfide or sodium hydrogen sulfide in the presence of an inert organic solvent, and subsequently acidifying. The 4-mercaptobenzonitriles thus accessible are new, with the exception of the unsubstituted 4-mercaptobenzonitrile, and can be used as intermediates for the preparation of nematic liquid-crystalline products, herbicides and plant-growth regulators.

摘要翻译： 通过在惰性有机溶剂的存在下使合适的4-卤代苄腈与硫化钠或硫化氢钠反应，然后酸化制备4-巯基苯腈。 因此可以使用的4-巯基苯腈是新的，除了未取代的4-巯基苄腈，可以用作制备向列型液晶产品，除草剂和植物生长调节剂的中间体。

公开(公告)号：US4814501A

公开(公告)日：1989-03-21

申请号：US138251

申请日：1987-12-28

申请人： Bruce E. Witzel ,  Robert K. Baker ,  Philippe L. Durette ,  Robert A. Frankshun

发明人： Bruce E. Witzel ,  Robert K. Baker ,  Philippe L. Durette ,  Robert A. Frankshun

IPC分类号： C07C319/14 ,  C07C323/62 ,  C07C333/04 ,  C07C149/41 ,  C07C102/06 ,  C07D213/62

CPC分类号： C07C319/14 ,  C07C323/62 ,  C07C333/04

摘要： Pyrolysis of substituted salicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)benzamide. Similarly, substituted 6-azasalicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)-6-aza-benzamide.

摘要翻译： 取代的水杨酸酯O（N，N-二烷基）硫代氨基甲酸酯的热解得到相应的N，N-二烷基-2-（甲硫基）苯甲酰胺。 类似地，取代的6-氮杂水杨酸O（N，N-二烷基）硫代氨基甲酸酯得到相应的N，N-二烷基-2-（甲硫基）-6-氮杂 - 苯甲酰胺。