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    • 5. 发明专利
    • Preparation of phospholipid long-chain alcohol derivative by enzymatic process
    • 通过酶法制备磷脂长链醇衍生物
    • JPS6188886A
    • 1986-05-07
    • JP20993184
    • 1984-10-08
    • Meito Sangyo Kk
    • KOKUSHO SUMITAKANAKAYAMA MINEOTSUNODA AKIRAKATO SHIGEAKIMACHIDA HARUOIWASAKI SHINJIRO
    • C07F9/10A61K9/127C12P7/02C12P7/40C12P7/62C12P9/00C12P13/00C12P13/02
    • A61K9/1271
    • PURPOSE: To obtain the titled phospholipid alcohol derivative such as phospholipid polyethylene glycol derivative, in high yield, by reacting a phospholipid with an alcohol in the presence of a phospholipase DM at specific temperature and pH.
      CONSTITUTION: A phospholipid of formula I {A is group of formula II or formu la III [R
      1 and R
      2 or -O-COR
      11 or -O-R
      12 (R
      11 and R
      12 are 1W21C aliphatic hydro carbon residue)]; A' is oxide anion or OH; B is -(CH
      2 )
      2 N
      + (CH
      3 )
      3 , -(CH
      2 )
      2 NH
      2 , etc.} is made to react with an alcohol compound at 60W70°C and about 7pH in the presence of a phospholipase DM. The alcoholic compound is a primary alcohol having ≥27C aliphatic or aromatic hydrocarbon residue (which may have substituent group such as halogen or an ether bond, etc. in the molecule) or a secondary alcohol compound having ≥11C alkyl residue which may be substituted with halogen, amino, etc.
      COPYRIGHT: (C)1986,JPO&Japio
    • 目的:通过在磷脂酶DM的存在下,在特定温度和pH下使磷脂与醇反应,以高产率获得标题磷脂醇衍生物如磷脂聚乙二醇衍生物。 构型:式I的磷脂(A是式II或式IIIIII的基团[R1和R2或-O-COR11或-O-R12(R11和R12是1-21C脂肪族氢碳残基)]; A'是氧化物阴离子或OH; 在磷脂酶DM存在下,B为 - (CH 2)2 N +(CH 3)3, - (CH 2)2 NH 2等)与醇化合物在60-70℃和约7pH反应。 醇化合物是具有> = 27C脂族或芳族烃残基(其分子中可具有取代基如卤素或醚键等)的伯醇或具有> = 11C烷基残基的仲醇化合物,其可以是 被卤素,氨基等取代
    • 9. 发明专利
    • Preparation of phospholipid heterocyclic compound derivative by enzymatic process
    • 通过酶学方法制备衍生的磷脂杂环化合物
    • JPS6188890A
    • 1986-05-07
    • JP20992984
    • 1984-10-08
    • Meito Sangyo Kk
    • KOKUSHO SUMITAKANAKAYAMA MINEOTSUNODA AKIRAKATO SHIGEAKIMACHIDA HARUOIWASAKI SHINJIRO
    • C12P17/00C12N9/16C12P17/02C12P17/04C12P17/06C12P17/10C12P17/12C12P17/14C12P17/18C12P19/02C12P19/30C12P19/32C12R1/01C12R1/03
    • Y02P20/52
    • PURPOSE: To produce the titled novel derivative which could not hitherto be produced, by reacting a specific phospholipid with a heterocyclic compound having a specific alcoholic OH group in the presence of a phospholipase DM.
      CONSTITUTION: A phospholipid of formula I {A is group of formula II or formu la III [R
      1 and R
      2 are -O-COR
      11 or -O-R
      12 (R
      11 is 7W21C aliphatic hydrocarbongroup); R
      12 is 1W21C aliphatic hydrocarbon group)]; A' is oxide anion or OH; B is -(CH
      2 )
      2 N
      + (CH
      3 )
      3 ), -(CH
      2 )
      2 NH
      2 , etc.}is made to react with a heterocyclic compound having an aloholic OH group in the presence of a phospholipase DM. The above OH group is (i) a reside of a heterocyclic primary alcohol compound having chain side group bonded to a primary alcoholic OH and having a heterocyclic group such as furan ring, (ii) a heterocyclic secondary alcohol compound residue having a heterocyclic group such as piperidine ring, or (iii) a (deoxy)pentose residue having pyridine ring, etc. as a substituent group.
      COPYRIGHT: (C)1986,JPO&Japio
    • 目的:在磷脂酶DM的存在下,通过使具体的磷脂与具有特定的醇OH基团的杂环化合物反应,生产迄今无法生产的标题新型衍生物。 构型:式I的磷脂(A是式II或式IIIIII的基团[R1和R2是-O-COR11或-O-R12(R11是7-21C脂族烃族基))。 R12为1-21C脂族烃基)]; A'是氧化物阴离子或OH; 在磷脂酶DM的存在下,B是 - (CH 2)2 N +(CH 3)3), - (CH 2)2 NH 2等与具有天然OH基团的杂环化合物反应。 上述OH基是(i)具有键侧基的杂环伯醇化合物与主要醇OH键合并具有杂环基的呋喃环,(ii)具有杂环基的杂环仲醇化合物残基如 作为哌啶环,或(iii)具有吡啶环的(脱氧)戊糖残基等作为取代基。