Phenylsilane → 2-Amino-5-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylic acid

HRID 869113노트

반응식

HRID 869113 반응식
[NH2:1][C:2]1[C:14]([C:15]([O:17]CC=C)=[O:16])=[C:5]2[N:6]=[C:7]([C:10]([F:13])([F:12])[F:11])[CH:8]=[CH:9][N:4]2[N:3]=1.C1([SiH3])C=CC=CC=1>C(Cl)Cl.C1C=CC([P]([Pd]([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)[P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)=CC=1>[NH2:1][C:2]1[C:14]([C:15]([OH:17])=[O:16])=[C:5]2[N:6]=[C:7]([C:10]([F:13])([F:11])[F:12])[CH:8]=[CH:9][N:4]2[N:3]=1

참가 물질

5

반응물 2

HCID 12752PhenylsilaneHCID 90417814Allyl 2-amino-5-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylate

생성물 1

HCID 904168892-Amino-5-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylic acid수율 56.7%

시약·촉매·용매 2

HCID 178418397HCID 178418397, 화합물촉매HCID 6344Dichloromethane용매

실험 절차

Allyl 2-amino-5-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylate 4a (240 mg, 0.8385 mmol) and phenylsilane (181.5 mg, 206.7 μL, 1.677 mmol) were dissolved in dry DCM (6 mL). Pd(PPh3)4 (38.76 mg, 0.03354 mmol) was added and the resulting solution was stirred at RT for 2 hrs. The suspension was filtered and the collected solid was washed with DCM (3×1 mL). The solid was dried under vacuum at 40° C. to yield compound 5a (117 mg, 56%).

후처리

  1. filtrationThe suspension was filtered
  2. washthe collected solid was washed with DCM (3×1 mL)
  3. customThe solid was dried under vacuum at 40° C.

출처 및 근거

ORD 기록
ord-aab874c5e59948c59ab3e5375e409aeb
출처 데이터셋
uspto-grants-2015_03
특허 번호
US08969360B2

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