Urea derivative and process for preparing the same
A process for preparing a compound (C) represented by the following formula: wherein R 1 represents hydrogen, C 1-6 alkyl or C 3-8 cycloalkyl, and R 2 represents hydrogen or methoxy, characterized by reacting a compound (A-1) represented by the following formula: wherein R 1 has the same definition as above, with a compound (B) represented by the following formula: wherein R 2 has the same definition as above, and L represents a leaving group, is provided. Compound (C) is effective for prevention or treatment of various diseases associated with angiogenesis neoplasia.
1. A process for preparing a compound (C) or a salt thereof represented by the following formula:
wherein R 1 represents hydrogen, C 1-6 alkyl or C 3-8 cycloalkyl, and wherein R 2 represents hydrogen or methoxy, said method comprising reacting a compound (A-1) represented by the following formula:
wherein R 1 has the same definition as above, with a compound (B) represented by the following formula:
wherein R 2 is defined as above, and L represents a leaving group.
2. A process according to claim 1 , wherein the reaction is performed in the presence of a base.
3. A process according to claim 2 , wherein the base is an alkali metal carbonate or an alkali metal alkoxide.
4. A process according to claim 2 , wherein the base is cesium carbonate, potassium carbonate or potassium t-butoxide.
5. A process according to claim 1 , wherein R 1 is hydrogen, methyl, ethyl, n-propyl or cyclopropyl.
6. A process according to claim 1 , wherein R 1 is cyclopropyl.
7. A process according to claim 1 , wherein R 2 is hydrogen.
8. A process according to claim 1 , wherein L is chlorine.
9. A process according to claim 1 , wherein the reaction is performed in dimethylsulfoxide in the presence of cesium carbonate or potassium t-butoxide.