5-[(3-amino-1-methyl-1H-indazol-6-yl)oxy]-3-(4-methoxybenzyl)-3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-one → 5-(3-Amino-1-methyl-1H-indazol-6-yloxy)-3,4-dihydro-1H-pyrido[2,3-d]pyrimidin-2-one

HRID 1045505

반응식

HRID 1045505 반응식
[NH2:1][C:2]1[C:10]2[C:5](=[CH:6][C:7]([O:11][C:12]3[C:21]4[CH2:20][N:19](CC5C=CC(OC)=CC=5)[C:18](=[O:31])[NH:17][C:16]=4[N:15]=[CH:14][CH:13]=3)=[CH:8][CH:9]=2)[N:4]([CH3:32])[N:3]=1>FC(F)(F)C(O)=O>[NH2:1][C:2]1[C:10]2[C:5](=[CH:6][C:7]([O:11][C:12]3[C:21]4[CH2:20][NH:19][C:18](=[O:31])[NH:17][C:16]=4[N:15]=[CH:14][CH:13]=3)=[CH:8][CH:9]=2)[N:4]([CH3:32])[N:3]=1

참가 물질

3

반응물 1

HCID 704971855-[(3-amino-1-methyl-1H-indazol-6-yl)oxy]-3-(4-methoxybenzyl)-3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-one

생성물 1

HCID 669262435-(3-Amino-1-methyl-1H-indazol-6-yloxy)-3,4-dihydro-1H-pyrido[2,3-d]pyrimidin-2-one수율 91.3%

시약·촉매·용매 1

HCID 6422Trifluoroacetic acid용매

반응 조건

온도
75 °C

실험 절차

Compound 276 (25.00 mg; 0.06 mmol; 1.00 eq.) was dissolved in trifluoroacetic acid (2.00 ml). The vessel was sealed and heated at 75 degrees C. for two days. The reaction was concentrated, redissolved in DMSO, treated with Et3N to get pH ˜8, and then purified via prep HPLC to afford 17mg (69%) of 277 as a white solid. LC-MS (M+H=311, obsd.=311).

후처리

  1. customThe vessel was sealed
  2. concentrationThe reaction was concentrated
  3. dissolutionredissolved in DMSO
  4. additiontreated with Et3N
  5. customto get pH ˜8
  6. custompurified via prep HPLC

출처 및 근거

ORD 기록
ord-5a7ae7da25594a88a6ea16db24a514cd
출처 데이터셋
uspto-grants-2013_10
특허 번호
US08569295B2

연결된 노트

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