Preparation method and application of suvorexant intermediate
An intermediate and reaction technology, which is applied in the field of preparation of Suwo Leisheng intermediates, can solve the problems of harsh reaction conditions, high risk factor, and difficulty in industrialization, and achieve the effect of mild reaction conditions, high safety factor, and easy control
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Embodiment 1
[0073] The preparation of embodiment 1 formula I compound
Embodiment 1-1
[0075]
Embodiment 1-1a
[0077] Add 16.0 g of N-tert-butoxycarbonyl-1,2-ethylenediamine and 14.0 mL of triethylamine into 200 mL of dichloromethane, slowly add 11.8 g of acetyl chloride dropwise, the reaction at room temperature is completed, and TLC until no N-tert Butoxycarbonyl-1,2-ethylenediamine. Water was added to quench the reaction, and the organic phase was separated, washed with water, dried, and filtered to obtain the organic phase, which was concentrated to dryness to obtain 19.1 g of the compound of formula I as a yellow liquid, with a yield of 94.6% and an HPLC purity of 97.8%.
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