9-ケトスピノシン誘導体

Japanese Patent JP2006517538

A

9-substituted keto-spinosyn derivatives (I) and their salts are new. 9-substituted keto-spinosyn derivatives of formula (I) and their salts are new. X = oxygen, NH or NR4; R1 = hydrogen or an amino sugar; R2 = hydrogen or, all optionally substituted, (cyclo)alkyl, (hetero)arylalkyl or (hetero)aryl, or when X = NH or NR4, COR' or CSR'; R' = amino, optionally substituted alkyl, (di)alkylamino, (hetero)aryl, (hetero)arylamino or (hetero)arylalkyl; R3 = hydrogen or hydroxy; R4 = optionally substituted alkyl, or with R2 it forms a 3 to 8-membered ring, optionally interrupted by one or more heteroatoms, such as oxygen sulfur, sulfinyl, sulfonyl, NH or NR5, and optionally substituted; R5 = (cyclo)alkyl, (hetero)arylalkyl or (hetero)aryl, all optionally substituted; A-B = CH=CH, CH=CMe, CH2CH2 or CH2CHMe Independent claims are also included for the following: (1) method for preparing (I) by reacting the corresponding 9-oxo compound (II) with NH2-XR2 in presence of base and optionally diluent; and (2) new intermediates of formula (II) where (i) R1 is group (1d) or (1e) and A-B is as defined above or (ii) R1 = group (1a) and A-B is other than CH=CH.

Martham, Olga
Rosel, peter
Beck, Michael A
Ebbing House-Kintscher, Ulrich
Fuerten, Roberto
Yes, Yu Peter
Maille, Walker
Frede, Rita
Ebertz, Guyunter

JP2006500529A

July 27, 2006

January 08, 2004

Click for automatic bibliography generation  

Bayer Crop Science Actien Gezershaft

C07D313/00; A01N43/10; A01N43/22; A01N43/40; A01N43/60; A01N43/713; A01N43/80; A01N47/20; A01N47/34; A61K31/365; A61K31/381; A61K31/41; A61K31/422; A61K31/427; A61K31/4427; A61K31/497; A61K31/7048; A61P33/14; A61P43/00; C07D315/00; C07D405/12; C07D409/12; C07D413/12; C07D417/12; C07H17/08; C07B53/00; C07B61/00

Yoshio Kawaguchi
Makoto Ono
Kenkyo Kanayama
Katsuma Osaki
Mitsuaki Tsubokura

Previous Patent: ＤＮＡ結合タンパク質の使用

Next Patent: 造影剤