Claims
- 1. A process for producing a pyridopyrimidine of the formula: comprising:(a) contacting a pyrimidine of the formula: with an alkylating agent of the formula R—X1 in the presence of an alkylating base under conditions sufficient to produce an alkylated pyrimidine of the formula: and(b) contacting said alkylated pyrimidine of Formula II-d with an aryl acetate of the formula Ar1—CH2—CO2R in the presence of a cyclization base under conditions sufficient to produce said pyridopyrimidine of Formula II-e or(a) contacting said pyrimidine of Formula II-c with said aryl acetate of the formula Ar1—CH2—CO2R in the presence of a cyclization base under conditions sufficient to produce a thiol pyridopyrimidine of the formula: and(b) contacting said thiol pyridopyrimidine of Formula III with said alkylating agent of the formula R—X1 in the presence of an alkylating base under conditions sufficient to produce said pyridopyrimidine of Formula II-e, wherein X1 is a leaving group; each R is independently alkyl; Ar1 is aryl.
- 2. The process of claim 1, wherein X1 is halide.
- 3. The process of claim 1 further comprising contacting said pyridopyrimidine of Formula II-e with a nitrogen alkylating agent of the formula R3—X2 under conditions sufficient to produce an N-substituted pyridopyrimidine of the formula: whereinR3 is alkyl, amino, monoalkylamino, dialkylamino, cycloalkyl, aralkyl, fluoroalkyl, heteroalkyl, cyanoalkyl, alkylene-C(O)—R′ (where R′ is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino) or acyl; X2 is a leaving group; and Ar1 and R are those defined in claim 1.
- 4. The process of claim 3, wherein X2 is a halogen.
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a divisional of U.S. patent application Ser. No. 09/943,338, filed Aug. 30, 2001 now U.S. Pat. No. 6,518,276 and claims the benefit of U.S. Provisional Application Nos. 60/229,577 and 60/229,584, filed concurrently on Aug. 31, 2000, which are incorporated herein by reference in their entirety. This patent application also incorporates by reference the entire disclosure of U.S. patent application. Ser. No. 09/943,407, entitled 7-Oxo-Pyridopyrimidines (I), filed on Aug. 30, 2001.
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Number |
Date |
Country |
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60/229577 |
Aug 2000 |
US |
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Aug 2000 |
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