Dichloromethane → (7R)-2-chloro-8-(1-cyclopropylethyl)-7-ethyl-5-methyl-7,8-dihydropteridin-6(5H)-one

HRID 44814

반응식

HRID 44814 반응식
Cl.[NH2:2][C@H:3]([CH2:8][CH3:9])[C:4](OC)=[O:5].[CH:10]1([C:13](=O)[CH3:14])[CH2:12][CH2:11]1.Cl[CH2:17]Cl.[Cl:19][C:20]1[N:25]=[C:24](Cl)[C:23]([N+:27]([O-])=O)=[CH:22][N:21]=1>ClCCCl>[Cl:19][C:20]1[N:25]=[CH:24][C:23]2[N:27]([CH3:17])[C:4](=[O:5])[C@@H:3]([CH2:8][CH3:9])[N:2]([CH:13]([CH:10]3[CH2:12][CH2:11]3)[CH3:14])[C:22]=2[N:21]=1

참가 물질

6

반응물 4

HCID 6344DichloromethaneHCID 13004Cyclopropyl methyl ketoneHCID 5212662,4-Dichloro-5-nitropyrimidineHCID 13283516methyl (2R)-2-aminobutanoate hydrochloride

생성물 1

HCID 58405334(7R)-2-chloro-8-(1-cyclopropylethyl)-7-ethyl-5-methyl-7,8-dihydropteridin-6(5H)-one

시약·촉매·용매 1

HCID 111,2-Dichloroethane용매

실험 절차

Intermediate SS is prepared from compound I-SS via compound II-SS, III-SS and IV-SS similarly to the methods used in preparing compound III-J, Intermediate J-1, compound IV-J and Intermediate J as described above, with (R)-methyl 2-aminobutanoate hydrochloride used instead of (R)-methyl 2-aminobutanoate and with cyclopropylethanone instead of dihydro-2H-pyran-4(3H)-one in the first step, and with PE/dichloromethane instead of PE/1,2-dichloroethane as solvent in the coupling of 2,4-dichloro-5-nitropyrimidine with compound II-SS. Compound III-SS; LCMS: 343.1 m/z (M+H)+. Compound IV-SS; LCMS: 281.1 m/z (M+H)+. Intermediate SS. LCMS: 295 m/z (M+H)+.

후처리

  1. customIntermediate SS is prepared from compound I-SS via compound II-SS, III-SS and IV-SS similarly to the methods

출처 및 근거

ORD 기록
ord-114beb85103a47df957a572d7b54baf4
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08541418B2

연결된 노트

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