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

HRID 869113ノート

反応式

HRID 869113 の反応式
[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

参加物

5

反応物 2

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

生成物 1

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

試薬・触媒・溶媒 2

HCID 178418397HCID 178418397、化合物触媒HCID 6344Dichloromethane溶媒

実験手順

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%).

後処理

  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.

出典と根拠

ORDレコード
ord-aab874c5e59948c59ab3e5375e409aeb
出典データセット
uspto-grants-2015_03
特許番号
US08969360B2

反応ノート

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