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    Production of N-substituted 2,7-dialkyl-4-hydroxy-5-amino-8-arly-octanoylamides
    4.
    发明授权
    Production of N-substituted 2,7-dialkyl-4-hydroxy-5-amino-8-arly-octanoylamides 失效

    公开(公告)号：US07009078B1

    公开(公告)日：2006-03-07

    申请号：US10048229

    申请日：2000-07-13

    申请人： Peter Herold ,  Stefan Stutz ,  Adriano Indolese

    发明人： Peter Herold ,  Stefan Stutz ,  Adriano Indolese

    IPC分类号： C07C233/04 ,  C07C233/05

    CPC分类号： C07D295/185 ,  C07C51/06 ,  C07C57/52 ,  C07C57/76 ,  C07C69/65 ,  C07C231/12 ,  C07C233/09 ,  C07C233/20 ,  C07C235/34 ,  C07C247/12 ,  C07D263/22 ,  C07C237/20

    摘要： From compounds of formula II wherein R1 and R2 are independently of one another H, C1–C6alkyl, C1–C6halogenalkyl, C1–C6alkoxy, C1–C6alkoxy-C1–C6alkyl, or C1–C6alkoxy-C1–C6alkyloxy, R3 is C1–C6alkyl, R4 is C1–C6alkyl, and R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6alkoxy-C1–C6-alkyl, C1–C6alkanoyloxy-C1–C6alkyl, C1–C6aminoalkyl, C1–C6alkylamino-C1–C6-alkyl, C1–C6-dialkylamino-C1–C6-alkyl, C1–C6-alkanoylamido-C1–C6-alkyl, HO(O)C—C1–C6-alkyl, C1–C6alkyl-O—(O)C—C1–C6alkyl, H2N—C(O)—C1–C6alkyl, C1–C6alkyl-HN—C(O)—C1–C6alkyl or (C1–C6alkyl)2N—C(O)—C1–C6-alkyl, R6 is C1–C6alkyl, R7 is C1–C6alkyl or C1–C6alkoxy, or R6 and R7 together are tetramethylene, pentamethylene, 3-oxa-1,5-pentylene or —CH2CH2O— substituted, if necessary, with C1–C4-Alkyl, phenyl or benzyl, it is possible—through halolactonization, azidation of the halogen group, ring opening with an amine R5—NH2, and reduction of the azide group to form the amino group—to prepare compounds of formula I wherein R5 is C1–C6alkyl, C1–C6hydroxyalkyl, C1–C6alkoxy-C1–C6alkyl, C1–C6alkanoyloxy-C1–C6alkyl, C1–C6aminoalkyl, C1–C6alkylamino-C1–C6alkyl, C1–C6dialkylamino-C1–C6-alkyl, C1–C6alkanoylamido-C1–C6alkyl, HO(O)C—C1–C6alkyl, C1–C6alkyl-O—(O)C—C1–C6alkyl, H2N—C(O)—C1–C6alkyl, C1–C6alkyl-HN—C(O)—C1–C6alkyl or (C1–C6alkyl)2—N—C(O)—C1–C6alkyl. If 2(S), 7(R)-diastereomer of formula II is used, the 2(S), 4(S), 5(S), 7(S)-diastereomer of formula Ia is obtained in a high degree of purity.

    Process for the preparing .alpha.-chloroacrylic acid chlorides
    10.
    发明授权
    Process for the preparing .alpha.-chloroacrylic acid chlorides 失效
    制备“氯丙烯酸氯化物”的方法

    公开(公告)号：US4066690A

    公开(公告)日：1978-01-03

    申请号：US724959

    申请日：1976-09-20

    申请人： Dieter-Bernd Reuschling ,  Harald Jensen

    发明人： Dieter-Bernd Reuschling ,  Harald Jensen

    IPC分类号： C07C51/62 ,  C07C57/76 ,  C07C51/58

    CPC分类号： C07C57/76 ,  C07C51/62

    摘要： .alpha.-Chloroacrylic acid chloride is obtained in a high yield by splitting off HCl from .alpha.,.beta.-dichloropropionic acid chloride at an increased temperature and under reduced pressure in the presence of a tertiary phosphine, a quaternary phosphonium salt or a tertiary phosphine oxide, sulfide, halide or imine. .alpha.-Chloroacrylic acid chloride is important as a starting and intermediate material for further syntheses, especially as the starting material for the total synthesis of prostaglandins according to Corey.