Claims
- 1. A process for producing a compound of formula (3): wherein R1, R2, R3, R4, and R5 are independently selected from the group consisting of a hydrogen atom, a hydroxyl group, an alkoxy group having 1 to 3 carbon atoms, an alkyl group having 1 to 3 carbon atoms, and a hydroxyalkyloxy group having 2 or 3 carbon atoms, wherein said process comprises:(a) converting a carboxyl group in a compound of formula (4) into a formyl group: wherein R1, R2, R3, R4, and R5 are as defined above, to obtain a compound of formula (2): wherein R1, R2, R3, R4, and R5 are defined as above; and (b) reductively alkylating aspartame with said compound of formula (2) and hydrogen in the presence of catalyst, to obtain said compound of formula (3).
- 2. The process of claim 1, wherein R2 is a hydroxyl group, R3 is a methoxy group, and R1, R4, and R5 are hydrogen atoms.
- 3. The process of claim 1, wherein said catalyst is selected from the group consisting of palladium carbon, platinum carbon, and mixtures thereof.
- 4. The process of claim 1, wherein said reductively alkylating is performed in a solvent which is selected from the group consisting of methanol, water, and mixtures thereof.
- 5. A process for producing a compound of formula (3): wherein R1, R2, R3, R4, and R5 are independently selected from the group consisting of a hydrogen atom, a hydroxyl group, an alkoxy group having 1 to 3 carbon atoms, an alkyl group having 1 to 3 carbon atoms, and a hydroxyalkyloxy group having 2 or 3 carbon atoms, wherein said process comprises:(a) reducing a double bond in a compound of formula (2): wherein R1, R2, R3, R4, and R5 are as defined above, to obtain a compound of formula (1): wherein R1, R2, R3, R4, and R5 are defined as above; and (b) reductively alkylating aspartame with said compound of formula (1) and hydrogen in the presence of catalyst, to obtain said compound of formula (3).
- 6. The process of claim 5, wherein R2 is a hydroxyl group, R3 is a methoxy group, and R1, R4, and R5 are hydrogen atoms.
- 7. The process of claim 5, wherein said catalyst is selected from the group consisting of palladium carbon, platinum carbon, and mixtures thereof.
- 8. The process of claim 5, wherein said reductively alkylating is performed in a solvent which is selected from the group consisting of methanol, water, and mixtures thereof.
- 9. A process for producing a compound of formula (3): wherein R1, R2, R3, R4, and R5 are independently selected from the group consisting of a hydrogen atom, a hydroxyl group, an alkoxy group having 1 to 3 carbon atoms, an alkyl group having 1 to 3 carbon atoms, and a hydroxyalkyloxy group having 2 or 3 carbon atoms, wherein said process comprises:(a) converting a carboxyl group in a compound of formula (4) into a formyl group: wherein R1, R2, R3, R4, and R5 are as defined above, to obtain a compound of formula (2): wherein R1, R2, R3, R4, and R5 are defined as above; (b) reducing a double bond in said compound of formula (2), to obtain a compound of formula (1): wherein R1, R2, R3, R4, and R5 are defined as above; and (c) reductively alkylating aspartame with said compound of formula (1) and hydrogen in the presence of catalyst, to obtain said compound of formula (3).
- 10. The process of claim 9, wherein R2 is a hydroxyl group, R3 is a methoxy group, and R1, R4, and R5 are hydrogen atoms.
- 11. The process of claim 9, wherein said catalyst is selected from the group consisting of palladium carbon, platinum carbon, and mixtures thereof.
- 12. The process of claim 9, wherein said reductively alkylating is performed in a solvent which is selected from the group consisting of methanol, water, and mixtures thereof.
- 13. A process for producing a compound of formula (3): wherein R1, R2, R3, R4, and R5 are independently selected from the group consisting of a hydrogen atom, a hydroxyl group, an alkoxy group having 1 to 3 carbon atoms, an alkyl group having 1 to 3 carbon atoms, and a hydroxyalkyloxy group having 2 or 3 carbon atoms, wherein said process comprises:(a) converting a carboxyl group in a compound of formula (5) into a formyl group: wherein R1, R2, R3, R4, and R5 are as defined above, to obtain a compound of formula (1): wherein R1, R2, R3, R4, and R5 are defined as above; and (b) reductively alkylating aspartame with said compound of formula (1) and hydrogen in the presence of catalyst, to obtain said compound of formula (3).
- 14. The process of claim 13, wherein R2 is a hydroxyl group, R3 is a methoxy group, and R1, R4, and R5 are hydrogen atoms.
- 15. The process of claim 13, wherein said catalyst is selected from the group consisting of palladium carbon, platinum carbon, and mixtures thereof.
- 16. The process of claim 13, wherein said reductive alkylating is performed in a solvent which is selected from the group consisting of methanol, water, and mixtures thereof.
- 17. A process for producing a compound of formula (3): wherein R1, R2, R3, R4, and R5 are independently selected from the group consisting of a hydrogen atom, a hydroxyl group, an alkoxy group having 1 to 3 carbon atoms, an alkyl group having 1 to 3 carbon atoms, and a hydroxyalkyloxy group having 2 or 3 carbon atoms, wherein said process comprises:(a) reducing a double bond in a compound of formula (4): wherein R1, R2, R3, R4, and R5 are as defined above, to obtain a compound of formula (5): wherein R1, R2, R3, R4, and R5 are defined as above; (b) converting a carboxyl group in said compound of formula (5) into a formyl group, to obtain a compound of formula (1): wherein R1, R2, R3, R4, and R5 are defined as above; and (c) reductively alkylating aspartame with said compound of formula (1) and hydrogen in the presence of catalyst, to obtain said compound of formula (3).
- 18. The process of claim 17, wherein R2 is a hydroxyl group, R3 is a methoxy group, and R1, R4, and R5 are hydrogen atoms.
- 19. The process of claim 17, wherein said catalyst is selected from the group consisting of palladium carbon, platinum carbon, and mixtures thereof.
- 20. The process of claim 17, wherein said reductively alkylating is performed in a solvent which is selected from the group consisting of methanol, water, and mixtures thereof.
Priority Claims (2)
Number |
Date |
Country |
Kind |
11-287398 |
Oct 1999 |
JP |
|
11-371284 |
Dec 1999 |
JP |
|
CROSS-REFERENCE TO A RELATED APPLICATION
The present application is a continuation application of PCT/JP00/06626 filed Sep. 26, 2000, the entire contents of which is incorporated by reference.
US Referenced Citations (3)
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EP |
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FR |
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Entry |
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Continuations (1)
|
Number |
Date |
Country |
Parent |
PCT/JP00/06626 |
Sep 2000 |
US |
Child |
10/117196 |
|
US |