Simple exploration of 5-Iodo-7H-pyrrolo[2,3-d]pyrimidin-4-amine

The synthetic route of 163622-50-2 has been constantly updated, and we look forward to future research findings.

Reference of 163622-50-2 , The common heterocyclic compound, 163622-50-2, name is 5-Iodo-7H-pyrrolo[2,3-d]pyrimidin-4-amine, molecular formula is C6H5IN4, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

Dissolve 3-iodo-4-amino-1H-pyrrole [3,4-d] pyrimidine (294 mg, 1.13 mmol) in 2 mL (1: 3) of a mixed solvent of ethanol and DME, and then add 0.25 mL of saturated sodium carbonate Solution andN-methyl 2-azaindole-3-boronic acid pinacol ester (413 mg, 1.6 mmol). After the whole system was ventilated three times, tetrakis (triphenylphosphine) palladium (127 mg, 0.11 mmol) was added to the mixture, and then the whole system was heated to 90 C. under nitrogen and stirred for 12 hours. After the reaction was completed, filtration was performed with celite, and the obtained filtrate was washed three times with water and dichloromethane. The organic phase was subjected to rotary evaporation under reduced pressure to obtain a solid, which was separated by silica gel column chromatography (eluent was dichloromethane containing 1-2% methanol), and finally 234 mg (0.88 mmol) of the target compound was obtained as a pale green solid. Yield: 78%.

The synthetic route of 163622-50-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Yaoya Science And Technology (Shanghai) Co., Ltd.; Liang Yonghong; Zeng Zhaosen; Ling Yuan; (35 pag.)CN110452243; (2019); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia