Title:
N-置換2,7-ジアルキル-4-ヒドロキシ-5-アミノ-8-アリール-オクタノイルアミドの製造
Document Type and Number:
Japanese Patent JP4922521
Kind Code:
B2
Abstract:
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.
Inventors:
Herolt, peter
Stutz, Stephan
Indreise, adriano
Stutz, Stephan
Indreise, adriano
Application Number:
JP2001514287A
Publication Date:
April 25, 2012
Filing Date:
July 13, 2000
Export Citation:
Assignee:
SPEEDEL PHARMA AG
International Classes:
C07C231/18; C07D307/33; C07B53/00; C07B61/00; C07C51/06; C07C57/52; C07C57/76; C07C67/343; C07C69/65; C07C231/12; C07C233/09; C07C233/20; C07C233/47; C07C235/34; C07C237/20; C07C237/22; C07C247/12; C07C259/06; C07D263/22; C07D263/26; C07D295/18; C07D295/185
Domestic Patent References:
| JP8081430A |
Other References:
J. Org. Chem.,(1989), Vol.54, No.5,p.1178-1185
Attorney, Agent or Firm:
Hajime Tsukuni
Fumio Shinoda
Fumio Shinoda