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44 条记录 (耗时 0.031 秒)

    4-(2-Pyridylamidoethyl)piperidines
    1.
    发明授权
    4-(2-Pyridylamidoethyl)piperidines 失效
    4-（2-吡啶基酰氨基乙基）哌啶

    公开(公告)号：US3992388A

    公开(公告)日：1976-11-16

    申请号：US623351

    申请日：1975-10-17

    申请人： Wayne E. Barth ,  Donald E. Kuhla

    发明人： Wayne E. Barth ,  Donald E. Kuhla

    IPC分类号： A61K31/445 ,  C07D213/82 ,  C07D401/12 ,  C07D213/56

    CPC分类号： C07D213/82 ,  A61K31/445 ,  C07D401/12 ,  Y10S514/866

    摘要： Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structue ##SPC1##Wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms.Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structue ##SPC2##With substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art.The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.

    摘要翻译： 本文公开了一种用于制备结构+ q，10的已知低血糖哌啶磺酰甲基脲的改进方法，其中R选自3-（2-甲氧基）吡啶基，3-（2-乙氧基）吡啶基和2-（ 4-氯）吡啶基和R'选自双环[2.2.1]庚-5-烯-2-基 - 内 - 甲基，双环[2.2.1]庚-2-基 - 内 - 甲基 ，7-氧杂二环[2.2.1]庚-2-基 - 甲基，1-金刚烷基和具有5-8个碳原子的环烷基。

    Process for the synthesis of 4-(2-pyridylamido ethyl) piperidines
    2.
    发明授权
    Process for the synthesis of 4-(2-pyridylamido ethyl) piperidines 失效
    合成4-（2-吡啶基酰氨基乙基）哌啶的方法

    公开(公告)号：US3933830A

    公开(公告)日：1976-01-20

    申请号：US504826

    申请日：1974-09-10

    申请人： Wayne E. Barth ,  Donald E. Kuhla

    发明人： Wayne E. Barth ,  Donald E. Kuhla

    IPC分类号： A61K31/445 ,  C07D213/82 ,  C07D401/12 ,  C07D211/02

    CPC分类号： C07D213/82 ,  A61K31/445 ,  C07D401/12 ,  Y10S514/866

    摘要： Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structure ##EQU1## wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms.Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structure ##EQU2## with substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art.The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.

    摘要翻译： 本文公开了一种改进的制备以下结构的已知降血糖哌啶磺酰胺的制备方法：OO PARALLEL PARALLEL R-CNH（CH 2）2 -SO 2 NHC-NHR'，其中R选自3-（2-甲氧基）吡啶基，3 - （2-乙氧基）吡啶基和2-（4-氯）吡啶基，R'选自双环[2.2.1]庚-5-烯-2-基 - 内 - 甲基，双环[2.2。 1]庚-2-基 - 内 - 甲基，7-氧杂双环[2.2.1]庚-2-基 - 甲基，1-金刚烷基和具有5-8个碳原子的环烷基。

    6-(Aminomethyl)penicillanic acid 1,1-dioxide esters and intermediates therefor
    3.
    发明授权
    6-(Aminomethyl)penicillanic acid 1,1-dioxide esters and intermediates therefor 失效
    6-（氨基甲基）青霉烷酸1,1-二氧化物酯及其中间体

    公开(公告)号：US4536393A

    公开(公告)日：1985-08-20

    申请号：US577478

    申请日：1984-02-06

    申请人： Wayne E. Barth

    发明人： Wayne E. Barth

    IPC分类号： A61K31/43 ,  C07D307/88 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D307/88 ,  C07D499/00

    摘要： 6-alpha- and 6-beta-(Aminomethyl)penicillanic acid, 1,1-dioxide esters which are hydrolyzable under physiological conditions, particularly those wherein the ester radical is 1H-isobenzofuran-3-on-1-yl or (5-methyl-1,3-dioxol-2-on-4-yl)methyl, and an improved process and intermediates used in their synthesis.

    摘要翻译： 6-α-和6-β-（氨基甲基）青霉烷酸，在生理条件下可水解的1,1-二氧化物酯，特别是其中酯基为1H-异苯并呋喃-3-基-1-基或（5- 甲基-1,3-二氧杂环戊烯-2-基-4-基）甲基，以及用于其合成的改进方法和中间体。

    Antibacterial 3-(5-tetrazolyl) penam compounds
    5.
    发明授权
    Antibacterial 3-(5-tetrazolyl) penam compounds 失效

    公开(公告)号：US4179511A

    公开(公告)日：1979-12-18

    申请号：US957197

    申请日：1978-11-01

    申请人： Wayne E. Barth

    发明人： Wayne E. Barth

    IPC分类号： C07D499/00 ,  A61K31/43

    CPC分类号： C07D499/00 ,  Y02P20/55

    摘要： Certain novel 6-acylamino-2,2-dimethyl-3-(5-tetrazolyl)penam derivatives, and salts thereof; their use as broad-spectrum antibacterial agents; and methods for their preparation. Their preparation comprises acylation of the novel intermediate, 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam or simple derivatives thereof, followed, in some cases, by further transformations of the 6-acylamino group or by removal of a protecting group from the 5-tetrazolyl moiety. Process for the preparation of 6-amino-2,2-dimethyl-3-(5-tetrazolyl)penam, simple derivatives thereof and intermediates therefor.

    3-Hydroxy and 3-acetoxy-6-triphenyl-methylaminopenams
    7.
    发明授权
    3-Hydroxy and 3-acetoxy-6-triphenyl-methylaminopenams 失效
    3-羟基和3-乙酰氧基-6-三苯基 - 甲基氨基戊二酸

    公开(公告)号：US4036846A

    公开(公告)日：1977-07-19

    申请号：US736811

    申请日：1976-10-29

    申请人： Wayne E. Barth

    发明人： Wayne E. Barth

    IPC分类号： A23K1/16 ,  C07D277/10 ,  C07D499/00 ,  C07F9/6561

    CPC分类号： C07F9/65611 ,  A23K20/116 ,  A23K20/137 ,  C07D277/10 ,  C07D499/00

    摘要： The present invention discloses novel 6-acylamino-2,2-dimethyl-3-phosphonopenams and certain lower alkyl esters thereof possessing antibacterial activity, methods for their production, and intermediates therefor; the production comprises the steps of reacting 6-triphenylmethylamino-2,2-dimethylpenam-3-carboxylic acid with lead tetraacetate to form the corresponding 3-acetoxy compound, the latter is converted to .alpha.-triphenylmethylamino-5,5-dimethyl-3-thiazoline-2-acetic acid which is condensed with dimethyl phosphite to produce .alpha.-triphenylmethylamino-5,5-dimethyl-4(0,0-dimethylphosphono)-thiazolidine-2-acetic acid which is cyclized to 6-triphenylmethylamino-2,2-dimethyl-3-(0,0-dimethylphosphono)penam and the latter is subsequently deblocked and acylated.

    摘要翻译： 本发明公开了具有抗菌活性的新颖的6-酰基氨基-2,2-二甲基-3-膦草丁酸及其某些低级烷基酯，其生产方法及其中间体; 该制备包括使6-三苯基甲基氨基-2,2-二甲基联苯-3-羧酸与四乙酸铅反应形成相应的3-乙酰氧基化合物的步骤，将其转化成α-三苯甲基氨基-5,5-二甲基-3- 与亚磷酸二甲酯缩合以产生α-三苯基甲基氨基-5,5-二甲基-4（0,0-二甲基膦酰基） - 噻唑烷-2-炔酸的4-噻唑啉-2-乙酸，将其环化为6-三苯基甲基氨基-2， 2-二甲基-3-（0,0-二甲基膦酰基）半缩醛，后者随后被去封闭并酰化。

    6-(1-carbamoyl-1-hydroxymethyl)penicillanic acid derivatives
    10.
    发明授权
    6-(1-carbamoyl-1-hydroxymethyl)penicillanic acid derivatives 失效
    6-（1-氨基甲酰基-1-羟甲基）青霉烷酸衍生物

    公开(公告)号：US4797394A

    公开(公告)日：1989-01-10

    申请号：US85675

    申请日：1987-06-05

    申请人： Wayne E. Barth

    发明人： Wayne E. Barth

    IPC分类号： C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/00

    摘要： 6-(1-Carbamoyl-1-hydroxymethyl)penicillanic acid derivatives are useful as antibacterials and/or beta-lactamase inhibitors.

    摘要翻译： PCT No.PCT / US85 / 02134 Sec。 371日期：1987年6月5日 102（e）1987年6月5日PCT 1985年10月29日PCT。6-（1-氨甲酰基-1-羟甲基）青霉烷酸衍生物可用作抗菌剂和/或β-内酰胺酶抑制剂。