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公开(公告)号:US4009159A
公开(公告)日:1977-02-22
申请号:US427232
申请日:1973-12-21
申请人: Takashi Kamiya , Yoshihisa Saito , Tsutomu Teraji , Osamu Nakaguti , Teruo Oku , Hitoshi Nakamura , Masashi Hashimoto
发明人: Takashi Kamiya , Yoshihisa Saito , Tsutomu Teraji , Osamu Nakaguti , Teruo Oku , Hitoshi Nakamura , Masashi Hashimoto
IPC分类号: C07D205/08 , C07D205/095 , C07D499/00 , C07D499/04 , C07D499/21 , C07D499/44 , C07D501/10 , C07D501/14 , C07D499/46 , C07D499/48 , C07D499/64
CPC分类号: C07D499/00 , C07D205/08 , C07D205/095
摘要: A penam derivative having the formula: ##STR1## wherein X represents a halogen atom, and wherein R.sub.1 represents an amino or acylamino, and R.sub.3 represents a radical selected from the group consisting of carboxy, ester, acid amide, acid anhydride, acid halide, and acid azide.
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公开(公告)号:US4007202A
公开(公告)日:1977-02-08
申请号:US547948
申请日:1975-02-07
申请人: Jan Verweij , Hong Sheng Tan
发明人: Jan Verweij , Hong Sheng Tan
IPC分类号: C07D205/08 , A61K31/545 , C07D201/02 , C07D205/095 , C07D207/46 , C07D209/48 , C07D401/12 , C07D403/12 , C07D501/08 , C07D501/10 , C07D501/30 , C07D501/60 , C07D207/12
CPC分类号: C07D209/48 , C07D207/46
摘要: Novel azetidine derivatives of the formula ##STR1## wherein R.sub.1 is an acylamido group, R.sub.2 is selected from the group consisting of ##STR2## wherein R.sub.4, R.sub.5 and R.sub.6 are individually selected from the group consisting of hydrogen, lower alkyl and lower alkenyl, n is 2 or 3 and -- in the case when formula IIB is a phenyl - this group may carry one to four substituents selected from the group consisting of halogen, lower alkyl, lower alkenyl and phenyl, and R.sub.3 is lower alkyl optionally substituted with 1 or 2 phenyls which phenyl groups may be substituted with nitro and the dotted lines of formula IIB indicate the optional presence of double bonds and a process for their preparation and process for the preparation of cephalosporanic acid derivatives using the azetidines of formula I as intermediates.
摘要翻译: 新颖的式Ⅰa的氮杂环丁烷衍生物,其中R 1是酰氨基,R 2选自其中R 4,R 5和R 6各自独立地选自下列的组合:IIA IIB IIC IID 由氢,低级烷基和低级烯基组成的组,n为2或3, - 在式IIB为苯基的情况下,该基团可以携带一至四个选自以下的取代基:卤素,低级烷基,低级 烯基和苯基,R3是任选被1或2个苯基取代的低级烷基,该苯基可以被硝基取代,式IIB的虚线表示双键的任选存在,以及它们的制备方法和制备方法 使用式I的氮杂环丁烷的头孢烷酸衍生物作为中间体。
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公开(公告)号:USB372016I5
公开(公告)日:1976-03-09
申请号:US37201673
申请日:1973-06-21
IPC分类号: C07D499/00 , C07D499/04 , C07D499/21 , C07D501/04 , C07D501/10 , C07D501/14 , C07D501/16
CPC分类号: C07D499/00
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公开(公告)号:USB442810I5
公开(公告)日:1976-02-24
申请号:US44281074
申请日:1974-02-14
IPC分类号: A61K31/545 , B01J27/00 , C07B61/00 , C07D20060101 , C07D205/00 , C07D279/00 , C07D401/04 , C07D499/04 , C07D501/10 , C07D501/22 , C07D501/28 , C07D501/30 , C07D501/34
CPC分类号: C07D499/00
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公开(公告)号:US3879398A
公开(公告)日:1975-04-22
申请号:US32321473
申请日:1973-01-12
申请人: GLAXO LAB LTD
IPC分类号: B01J31/02 , C07D499/00 , C07D501/10 , C07F9/38 , C07D31/24 , C07D31/26 , C07D31/44 , C07D31/46
CPC分类号: B01J31/0239 , B01J31/0244 , B01J31/0259 , C07D499/00 , C07F9/38 , C07F9/3808
摘要: The invention relates to a process for the preparation of 7 Beta -acylamido-3-methylceph-3-em-4-carboxylic acid esters from 6 Beta -acylamido penicillanic acid 1-oxide esters in the presence of catalysts which are salts or complexes of acids with nitrogen bases having a pKb of not less than 4. The salts or complexes may be formed in situ.
摘要翻译: 本发明涉及一种在催化剂存在下从6β-酰基酰胺青霉烷酸1-氧化物酯制备7β-酰氨基-3-甲基头孢-3-烯-4-羧酸酯的方法,该催化剂是 具有pKb不低于4的氮碱的酸。盐或络合物可以原位形成。
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公开(公告)号:US3714146A
公开(公告)日:1973-01-30
申请号:US3714146D
申请日:1970-10-05
申请人: BRISTOL MYERS CO
发明人: GOTTSTEIN W , CHENEY L
IPC分类号: C07D501/04 , A61K20060101 , A61K31/545 , A61K31/546 , C07D20060101 , C07D499/80 , C07D501/10 , C07D501/22 , C07D501/58 , C07D501/60 , C07G11/00 , C07D99/16 , C07D99/24
CPC分类号: C07D501/22 , C07D501/58 , Y02P20/55
摘要: The antibacterial agent cephalexin is prepared from readily available hetacillin by the consecutive steps of nitrosation or formylation to give N-nitroso- or N-formyl-hetacillin, oxidation as with NaIO4 below pH 5 to give the corresponding sulfoxide, rearrangement by heat, preferably with acid present, to give Nnitroso- or N-formylhetacephalexin and finally cleavage to give cephalexin as by zinc and acetic acid or Raney nickel and hydrogen or, preferably, hydrogen chloride in dioxane.
摘要翻译: 抗菌剂头孢氨苄通过亚硝化或甲酰化的连续步骤由容易获得的赫曲西林制备得到N-亚硝基或N-甲酰基 - 赫曲西林,用低于pH 5的NaIO 4进行氧化,得到相应的亚砜,加热重排,优选用 酸,存在,得到N-亚硝基或N-甲酰基蝶呤,最后裂解,得到头孢氨苄,如锌和乙酸或阮内镍和氢,或优选氯化氢在二恶烷中。
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公开(公告)号:US3705892A
公开(公告)日:1972-12-12
申请号:US3705892D
申请日:1970-09-14
申请人: LILLY CO ELI
发明人: COOPER ROBIN D G
IPC分类号: C07D499/00 , C07D501/10 , C07D91/14
CPC分类号: C07D499/00
摘要: TREATMENT OF A PENICILLIN SULFOXIDE WITH A TRIPHENYL PHOSPHINE OR TRIALKYL PHOSPHITE RESULTS IN REARRANGEMENT TO A THIAZOLINE AZETIDINONE, THIS REARRANGEMENT PRODUCT CAN THEN BE CONVERTED TO A CEPHALOSPORIN OR TO A DIFFERENT PENICILLIN.
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公开(公告)号:US3668202A
公开(公告)日:1972-06-06
申请号:US3668202D
申请日:1970-02-24
申请人: LILLY CO ELI
IPC分类号: C07D501/10 , C07D501/14 , C07D99/24 , C07D99/14
CPC分类号: C07D501/10
摘要: Preparing a 3-hydroxy-3-methyl-cepham-4-carboxylic acid, salt or ester in improved yields by heating a penicillin sulfoxide acid, salt, or ester in the presence of sulfuric or sulfamic acid, or a salt or ester thereof in a solvent system containing a tertiary carboxamide.
摘要翻译: 在硫酸或氨基磺酸或其盐或酯的存在下,通过加热青霉素亚砜酸,盐或酯来制备3-羟基-3-甲基 - 头孢烯-4-羧酸盐或酯, 含有叔甲酰胺的溶剂体系。
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公开(公告)号:US3275626A
公开(公告)日:1966-09-27
申请号:US21358862
申请日:1962-07-31
申请人: LILLY CO ELI
发明人: MORIN ROBERT B , JACKSON BILLY G
IPC分类号: C07D499/00 , C07D499/44 , C07D501/10
CPC分类号: C07D499/00
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