- Preparation method of ceftobiprole intermediate (R)-1-benzyl-3-aminopyrrolidine
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The invention discloses a preparation method of a ceftobiprole intermediate, namely (R)-1-benzyl-3-aminopyrrolidine. The preparation method specifically comprises the following steps: with D-asparticacid as an initial raw material, carrying out amino protection, esterification, reduction, bromination cyclization and 3-amino protection removal successively to obtain (R)-1-benzyl-3-aminopyrrolidine. According to the method, the defects that raw materials for preparing (R)-1-benzyl-3-aminopyrrolidine are expensive, high temperature and high pressure are needed, precious metal is used for catalysis and the like in the prior art are overcome. All the materials used in the invention are cheap and easily available, so cost is low; and reactions can be carried out at normal temperature, so energyconsumption is low, industrial production is facilitated, and pollution is small.
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- A kind of optical active pharmaceutical process for the preparation of intermediates
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The invention relates to a preparation method of an optical active compound, represented by formula I, or a hydrochloride of the optical active compound by taking a compound with optical activity as a starting material. Raw materials of the preparation method are cheap and easily available; no splitting is needed; the whole technological operation is simple and convenient; cost is low; pollution on environment is less; and the preparation method is suitable for industrialized production. In the formula I, n is 1 or 2 or 3.
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Paragraph 0054; 0055
(2016/10/17)
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