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8H-Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, 2-(2-furanyl)- synthesis

4synthesis methods
N-(6-amino-1H-pyrazolo[3,4-d]pyrimidin-4-yl)furan-2-carbohydrazide

377729-81-2
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8H-Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine, 2-(2-furanyl)-

321661-12-5
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Yield:321661-12-5 83%

Reaction Conditions:

with N,O-bis-(trimethylsilyl)-acetamide;1,1,1,3,3,3-hexamethyl-disilazane at 110;

Steps:

1.B Step B: 2- (furan-2-yl) -7H-pyrazolo [4, 3-e] [1, 2, 4] triazolo [1, 5-c] pyrimidin-5-amine

A solution of N'- (6-amino-1H-pyrazolo [3, 4-d] pyrimidin-4-yl) furan-2-carbohydrazide (17 g, 65 mmol) in BSA (136 mL) and HMDS (160 mL) was heated at 110 overnight. The solution was concentrated at 60 under reduced pressure. The residue was added with water (200 mL) and slurried for 1 hr. The solid was filtered, washed with water and dried to obtain the desired product as a brown solid (13.1 g, 83%) . MS: M/e 242 (M+1) +.

References:

WO2019/196803,2019,A1 Location in patent:Paragraph 0105; 0109