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Method For Producing Pyrazine Carboxamide Compound And Synthetic Intermediate Thereof
Abstract: [Problem] To provide: a novel method for producing a pyrazine carboxamide compound as a production material of pharmaceutical products etc.; and a synthetic intermediate that is useful in said production method. [Solution] As a result of diligent research on production methods in industrially producing a pyrazine carboxamide compound the inventors have found that by using a predetermined material and synthetic intermediate a pyrazine carboxamide compound can be produced according to a method that is suitable for industrial production as a pharmaceutical product does not require purification by silica gel column chromatography and in which overall yield is greatly improved thus accomplishing the present invention.
Notices, Deadlines & Correspondence
Patent Information
Applicants
ASTELLAS PHARMA INC.
Inventors
1. AKIBA, Takahiro
2. HOSHII, Hiroaki
3. SHIMADA, Itsuro
4. KOMENOI, Kousuke
5. NISHIKAWA, Kentaro
6. MORINAGA, Yasuhiro
Specification
Claims
[Claim 1] A method for producing a compound of the formula (1) or a salt thereof
[Chem. 1]
comprising reacting a compound of the formula (2) or a salt thereof [Chem. 3]
with a base under dehydrochlorination reaction conditions.
[Claim 2] The production method according to claim 1, wherein the compound of
5 the formula (2) or the salt thereof is produced by a production method comprising reacting a compound of the formula (3) or a salt thereof [Chem. 4]
with 3-chloropropanoyl chloride under acylation reaction conditions.
28
[Claim 3] The production method according to claim 2, wherein the compound of
the formula (3) or the salt thereof is produced by a production method comprising reacting a compound of the formula (4) or a salt thereof [Chem. 5]
5
n
under deprotection reaction conditions.
10 [Claim 4] The production method according to claim 3, wherein the compound of
the formula (4) or the salt thereof is produced by a production method comprising reacting a compound of the formula (6) or a salt thereof [Chem. 6]
15
with a compound of the formula (5) or a salt thereof [Chem. 7]
20
under aromatic nucleophilic substitution reaction conditions.
[Claim 5] The production method according to claim 4, wherein the compound of
2 5 the formula (6) or the salt thereof is produced by a production method comprising reacting
a compound of the formula (8) or a salt thereof
29
[Chem. 8]
5 with a compound of the formula (7) or a salt thereof [Chem. 9]
0 in 2-butanol in the presence of a base under aromatic nucleophilic substitution reaction conditions at 80°C to 90°C.
[Claim 6] A method of producing a compound of the formula (9)
[Chem. 10]
5
comprising reacting the compound of the formula (1) or the salt thereof produced by the method according to any one claims 1 to 5 with methanesulfonic acid to form 0 monomethanesulfonate.
[Claim 7] A compound of the formula (2) or a salt thereof
[Chem. 3]
30
[Claim 8] The production method according to claim 1, comprising a step of
removing a portion of impurities contained in a crude compound of the compound of the 5 formula (1) by treating a solution containing the crude compound with activated carbon.
[Claim 9] The production method according to claim 6, wherein a mixed solvent of
acetone and dimethylsulfoxide is used as a reaction solvent.
31
Documents
Application Documents
| # | Name | Date |
|---|---|---|
| 1 | 201747026495-TRANSLATIOIN OF PRIOIRTY DOCUMENTS ETC. [26-07-2017(online)].pdf | 2017-07-26 |
| 2 | 201747026495-STATEMENT OF UNDERTAKING (FORM 3) [26-07-2017(online)].pdf | 2017-07-26 |
| 3 | 201747026495-PRIORITY DOCUMENTS [26-07-2017(online)].pdf | 2017-07-26 |
| 4 | 201747026495-POWER OF AUTHORITY [26-07-2017(online)].pdf | 2017-07-26 |
| 5 | 201747026495-FORM 1 [26-07-2017(online)].pdf | 2017-07-26 |
| 6 | 201747026495-DECLARATION OF INVENTORSHIP (FORM 5) [26-07-2017(online)].pdf | 2017-07-26 |
| 7 | 201747026495-COMPLETE SPECIFICATION [26-07-2017(online)].pdf | 2017-07-26 |
| 8 | 201747026495-CLAIMS UNDER RULE 1 (PROVISIO) OF RULE 20 [26-07-2017(online)].pdf | 2017-07-26 |
| 9 | 201747026495.pdf | 2017-08-01 |
| 10 | 201747026495-Proof of Right (MANDATORY) [05-09-2017(online)].pdf | 2017-09-05 |
| 11 | Correspondence by Agent_Form1_07-09-2017.pdf | 2017-09-07 |
| 12 | 201747026495-FORM 3 [31-10-2017(online)].pdf | 2017-10-31 |