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6-BOC-3-AMINO-5,6,7,8-TETRAHYDRO-[1,6]NAPHTHYRIDINE synthesis

2synthesis methods
-

Yield: 93.37%

Reaction Conditions:

with palladium on activated charcoal;hydrogen in methanol at 15 - 20; under 2068.65 Torr; for 16 h;

Steps:

19.B
Step B: Pd/C (1.00 g) was added to a solution of t-butyl 3-nitro-7,8-dihydro-5H-1,6-naphthyridine-6-carboxylate (3g, 10.74 mmol, 1 eq.) in methanol (100 mL) at room temperature under hydrogen gas environment (40 Psi). Thereaction solution was stirred at room temperature for 16 hours. After the completion of the reaction, the reactionsolution was filtrated and concentrated to give t-butyl 3-amino-7,8-dihydro-5H-1,6-naphthyridine-6-carboxylate (2.5g, 10.03 mmol, 93.37% yield) as a white solid

References:

Chia Tai Tianqing Pharmaceutical Group Co., Ltd.;CHEN, Shuhui;DING, Charles Z.;YAN, Xiaobing;HUANG, Wei;HU, Guoping;LI, Jian;ZHANG, Xiquan;YANG, Ling;XU, Hongjiang EP3248968, 2017, A1 Location in patent:Paragraph 0092

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