- Preparation method of loteprednol etabonate
-
The invention provides a preparation method of loteprednol etabonate. The preparation method comprises the following steps: (1) N-arylation reaction: carrying out a reaction on a compound I with an iodobenzene analogue under an alkaline condition to obtain a compound shown as a formula II; 2) elimination reaction: carrying out a reaction on the compound shown in the formula II with an ethylene oxide analogue in methanol under an alkaline condition to obtain a compound shown in a formula III; 3) esterification reaction: carrying out a reaction on the compound shown in the formula III with ethylchloroformate under an organic alkaline condition to obtain a compound shown in a formula IV; and 4) chlorination reaction: carrying out chlorination reaction on the compound in the formula IV underthe action of potassium persulfate to obtain the loteprednol etabonate. In the reaction route, the cheap and readily available compound I is used as a starting raw material, so that the process conditions are mild, the synthesis steps are simplified, the dosage of toxic reagents is reduced, and the yield is relatively high.
- -
-
-
- Loteprednol preparation method and ophthalmic composition of loteprednol
-
The present invention relates to a loteprednol preparation method and an ophthalmic composition of loteprednol, particularly to a loteprednol preparation method, which comprises: dissolving a raw material loteprednol in a first organic solvent to obtain a drug-containing solution, adding a second organic solvent to the obtained solution in a dropwise manner under stirring, continuously stirring, filtering, washing the filter cake by using the second organic solvent, and drying the obtained filter cake in a vacuum oven to obtain the product. The invention further provides a loteprednol bulk drug prepared according to the method, an ophthalmic pharmaceutical composition prepared by using the prepared loteprednol as a bulk drug, and uses of the prepared loteprednol in preparation of drugs for treatment or prevention of ocular inflammations or dry eye. The method of the present invention has excellent pharmaceutical properties, wherein the prepared bulk drug and the preparation have excellent stability.
- -
-
-
- A method for synthesizing loteprednol etabonate and a method for synthesizing intermediate (by machine translation)
-
The present invention provides a method of synthesizing loteprednol etabonate, comprises the following steps: step 1: to prednisolone as raw material preparation 11 β, 17 α - dihydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid; step 2: adopts the 11 β, 17 α - dihydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid preparation 17 α - ((ethoxy-formyl) oxy) - 11 β - hydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid ethyl carbonic anhydride; step 3: the 17 α - ((ethoxy-formyl) oxy) - 11 β - hydroxy - 3 - oxo male steroid - 1, 4 - diene - 17 β - carboxylic acid ethyl carbonic anhydride adding ethanol into sodium after a period of time by adding chlorine iodine methane then will be chlorine iodine methane. In step 3 can avoid the influence of the introduction of water to the intermediate. (by machine translation)
- -
-
Paragraph 0025; 0031; 0032
(2017/05/05)
-
- Method for reducing or preventing transplant rejection in the eye and intraocular implants for use therefor
-
Methods for reducing or preventing transplant rejection in the eye of an individual are described, comprising: a) performing an ocular transplant procedure; and b) implanting in the eye a bioerodible drug delivery system comprising an immunosuppressive agent and a bioerodible polymer.
- -
-
-