A kind of synthetic method of 5-biphenyl-4-amino-2-methylpentanoic acid intermediate
A synthesis method and biphenyl technology, applied in the field of medicine, can solve the problems of poor methylation selectivity, low yield, difficult separation of diastereomers, etc., and achieve good selectivity and solve the problem of poor reaction selectivity. Effect
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Embodiment 1
[0069] Synthesis of compound (5a)
[0070]
[0071] Add 288g of compound 6 into 1.5L of dichloromethane, add 476g of p-toluenesulfonyl chloride and 25g of DMAP, drop the temperature to 0°C, add 610g of triethylamine dropwise, and stir at room temperature for 3 hours after dropping. The reaction solution was washed with water, washed with acid, dried, concentrated, and slurried by adding methyl tert-butyl ether to obtain 545 g of compound 5a.
Embodiment 2
[0073] Synthesis of compound (4a)
[0074]
[0075] Add 190g of 5a into 1L of ethyl acetate, add 169g of Boc-anhydride, 8.7g of DMAP, and heat to 50°C for 5 hours. The reaction solution was washed with water, dried and concentrated to obtain 243 g of compound 4a, with a yield of 96.4%.
Embodiment 3
[0077] Synthesis of compound (4b)
[0078]
[0079] 190g of 5a was added to 1L of ethyl acetate, 8.7g of DMAP and 86g of triethylamine were added, 94g of pivaloyl chloride was added dropwise at 0°C, and the reaction was completed for 3 hours. The reaction solution was washed with water, washed with acid, dried and concentrated to obtain 235 g of compound 4a with a yield of 93.6%.
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