Process for preparing acetoxyazetidinone derivative and intermediate
thereof
    55.
    发明授权
    Process for preparing acetoxyazetidinone derivative and intermediate thereof 失效
    制备乙酰氧基氮杂环丁酮衍生物及其中间体的方法

    公开(公告)号:US5831091A

    公开(公告)日:1998-11-03

    申请号:US743834

    申请日:1996-11-05

    摘要: An N-�2-(1-hydroxyethyl)-3-oxopropyl!amine compound of the formula �III!: ##STR1## wherein Ring B represents a benzene ring which may be substituted; W represents oxygen atom or sulfur atom; Y represents oxygen atom, sulfur atom or N R.sup.0, R.sup.0 represents hydrogen atom or a substituent; Z represents a substituted methylene group which contains at least one chiral center; R.sup.5 represents an aralkyloxycarbonyl group or an alkoxycarbonyl group; R.sup.6 represents hydrogen atom, an aralkyl group, an acyloxy group, a tri-substituted silyloxy group or an alkoxy group; or both of R.sup.5 and R.sup.6 bond at their termini and combine with the adjacent nitrogen atom to form phthalimido group, and a process thereof are disclosed. Said compound �III! is useful as a starting compound of .beta.-lactam antibacterial agents.

    摘要翻译: 式[III]的N- [2-(1-羟乙基)-3-氧代丙基]胺化合物:其中环B表示可被取代的苯环; W表示氧原子或硫原子; Y表示氧原子,硫原子或N R0,R0表示氢原子或取代基; Z表示含有至少一个手性中心的取代亚甲基; R5表示芳烷氧基羰基或烷氧基羰基; R6代表氢原子,芳烷基,酰氧基,三取代甲硅烷氧基或烷氧基; 或者R 5和R 6两者在其末端键合并与相邻的氮原子结合形成苯二甲酰亚氨基,并且公开了其方法。 所述化合物[III]可用作β-内酰胺抗菌剂的起始化合物。

    Process for the preparation of cyclohexyl-azetidinones
    56.
    发明授权
    Process for the preparation of cyclohexyl-azetidinones 失效
    环己基 - 氮杂环丁酮的制备方法

    公开(公告)号:US5817806A

    公开(公告)日:1998-10-06

    申请号:US704758

    申请日:1997-01-03

    IPC分类号: B01J31/02 C07D205/08 C07F7/18

    摘要: 1. A process for the preparation of compounds of formula (I) wherein R.sub.1 is a hydroxyl protecting group ##STR1## which comprises reacting the azetidinone (II) with the homochiral (2S)-2- methoxycyclohexane (III) or the complex thereof formed with one molecule of stannic chloide. ##STR2##

    摘要翻译: PCT No.PCT / EP95 / 01114 Sec。 371日期1997年1月3日 102(e)日期1997年1月3日PCT 1995年3月23日PCT公布。 WO95 / 26333 PCT出版物 (I)化合物的制备方法,其中R1是羟基保护基团(I),其包括使氮杂环丁酮(II)与同基因(2S)-2-甲氧基环己烷 (III)或其与一分子的四核苷酸形成的络合物。 (二)(三)

    Process for the production of 4-substituted azetidinone derivative
    57.
    发明授权
    Process for the production of 4-substituted azetidinone derivative 失效
    用于制备4-取代的氮杂环丁酮衍生物的方法

    公开(公告)号:US5792861A

    公开(公告)日:1998-08-11

    申请号:US743327

    申请日:1996-11-04

    摘要: The present invention provides a process for the production of a 4-substituted azetidinone. The process comprises reacting ##STR1## wherein R represents a hydrogen atom or a protecting group for N, R.sup.1 represents an alkyl which may be a substituent having an unprotected or protected hydroxyl group; and Z represents a leaving group; with ##STR2## wherein R.sup.2 represents hydrogen or alkyl, R.sup.3 and R.sup.4 each represent hydrogen, alkyl, alkenyl, alkynyl, phenyl, cycloalkyl, or naphthyl, or R.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a ring system; X and Y each represent oxygen, sulfur or N-r.sup.1, wherein r.sup.1 represents a hydrogen atom or lower alkyl; A, B, D and E each represent nitrogen or C-r.sup.2, wherein r.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy, provided that at least two of A, B, D and E are C-r.sup.2 ; and a ring involving G, J and K has two carbon/carbon double bonds therein and one of G, J and K represents oxygen, sulfur or N-r.sup.1 while the remaining two represent C-r.sup.2 ; in the presence of M(Hal).sub.n (R.sup.5).sub.m (V) wherein M represents a metal atom; Hal represents halogen; R.sup.5 represents lower alkyl, lower alkoxy, phenoxy, substituted phenoxy or cyclopentadienyl; and n and m are each 0, 1, 2, 3, 4 or 5, provided that n+m stands for the valence of M; and a base to thereby give: ##STR3##

    摘要翻译: 本发明提供了制备4-取代的氮杂环丁酮的方法。 该方法包括使其中R表示氢原子或N为保护基的化合物(III)反应,R 1表示可以是具有未被保护或被保护的羟基的取代基的烷基; Z表示离去基团; 代表氢或烷基,R3和R4各自表示氢,烷基,烯基,炔基,苯基,环烷基或萘基,或R3和R4与它们所键合的碳原子一起形成环系; X和Y各自表示氧,硫或N-r1,其中r1表示氢原子或低级烷基; A,B,D和E各自表示氮或C-R 2,其中R 2表示氢,卤素,低级烷基或低级烷氧基,条件是A,B,D和E中的至少两个为C-R 2; 涉及G,J和K的环在其中具有两个碳/碳双键,G,J和K之一表示氧,硫或N-r1,其余两个表示C-r2; 在M(Hal)n(R5)m(V)的存在下,其中M表示金属原子; 卤代表卤素; R5表示低级烷基,低级烷氧基,苯氧基,取代的苯氧基或环戊二烯基; n和m分别为0,1,2,3,4或5,条件是n + m代表M的化合价; (II-1)或(II-2)所示的基础,从而得到: