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The invention discloses a method for synthesizing chiral morpholine from propargyl alcohol ester. Chiral morpholine is an important drug molecular skeleton and is widely applied to the aspects of analgesia, anesthesia, tumor resistance, heart treatment and the like as a drug active ingredient, but an efficient synthesis method is lacked. According to the method disclosed by the invention, under the regulation and control of arylboronic acid and a specific chiral ligand, propargyl alcohol ester and an affinity reagent react to obtain optically pure (87-97% ee) morpholine. The method has the characteristics that the catalyst and the ligand are wide in source, and the substrate is cheap and easy to obtain; the chiral morpholine has excellent enantioselectivity and good functional group compatibility, can be suitable for structural modification of bioactive molecules and intermediates, and is a simple and efficient asymmetric catalysis strategy for synthesizing chiral morpholine.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a cetrorelix acetate preparation composition for injection and a preparation method thereof.According to the preparation composition, through a specific freeze-drying process including a slow freezing stage, an annealing stage, primary drying and secondary drying, it is effectively guaranteed that the in-batch quality uniformity of a preparation is good, and the long-term stability is excellent; and industrial mass production is facilitated.

The invention discloses a method for synthesizing a non-cyclic and non-terminal vicinal diol derivative based on propargyl alcohol ester. Through a coupling strategy that propargyl alcohol ester and an exogenous nucleophilic reagent are catalyzed by transition metal (palladium), construction of a bimolecular exogenous nucleophilic group substituted allyl skeleton is realized. The strategy breaks through the dilemma that alkenylation products are limited to construction of cyclic molecules at the present stage and the tail ends of the alkenylation products are limited, and a reform synthesis scheme is provided for selective conversion of propargyl alcohol ester catalyzed by transition metal. The selected catalyst and ligand are wide in source, and the substrate is cheap and easy to obtain; the method provided by the invention has the advantages of high selectivity, excellent stereoselectivity and good functional group compatibility, can be suitable for structural modification of bioactive molecules and intermediates, is a simple and efficient asymmetric catalysis strategy for synthesizing non-cyclic and non-terminal vicinal diol derivatives, and has a good application prospect.