76-25-5Relevant articles and documents
Synthesis, pharmacokinetics, efficacy, and rat retinal toxicity of a novel mitomycin C-triamcinolone acetonide conjugate
Macky, Tamer A.,Oelkers, Carsten,Rix, Uwe,Heredia, Martin L.,Künzel, Eva,Wimberly, Mark,Rohrer, Baerbel,Crosson, Craig E.,Rohr, Jürgen
, p. 1122 - 1127 (2002)
A novel conjugate of mitomycin C (MMC) and triamcinolone acetonide (TA) was synthesized using glutaric acid as a linker molecule. To determine the rate of hydrolysis, the conjugate was dissolved in aqueous solution and the rate of appearance of free MMC and TA was determined by high-performance liquid chromatography analysis. Antiproliferative activity of the MMC-TA conjugate and parent compounds was assessed using an NIH 3T3 fibroblast cell line. Cell growth was quantified using the MTT assay. Kinetic analysis of the hydrolysis rate demonstrated that the conjugate had a half-life of 23.6 h in aqueous solutions. The antiproliferative activities of the MMC-TA conjugate and MMC were both concentration dependent, with similar IC50 values of 2.4 and 1.7 μM, respectively. However, individual responses at concentrations above 3 μM showed that the conjugate was less active than MMC alone. TA alone showed only limited inhibition of cell growth. Studies evaluating intravitreal injection of the conjugate demonstrate that this agent produced no measurable toxicity. Our data provide evidence that the MMC-TA conjugate could be used as a slow-release drug delivery system. This could in turn be used to modulate a posttreatment wound healing process or to treat various proliferative diseases.
Preparation method of triamcinolone acetonide
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Paragraph 0023; 0025; 0030-0031; 0036-0037; 0042, (2021/10/11)
The preparation method comprises the following steps: an oxidation reaction, a hydrolysis reaction, an epoxy reaction and a fluorine-containing reaction. After formic acid is added to the organic solvent acetone, a certain amount of the oxidant potassium permanganate is added after formic acid is added, and after the thin layer is analyzed to no raw material, a certain amount of the reducing liquid is added into the reactor, and after the reaction is complete, a certain amount of water is added, and after the reaction is complete 55 - 65min, the oxide is obtained by suction filtration. The method is mild in reaction condition, easy to control and small in auxiliary material toxicity. The preparation method adopts the transformation of 9, 11-position, 16,17-position and 21-position, can obtain triamcinolone, adopts the company existing products as starting materials, is short in route, easily available in raw materials, free of auxiliary materials with strong toxicity, high in yield and low in cost.
Synthetic method for preparing 16,17 ketal
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Paragraph 0035-00, (2020/04/06)
The invention relates to a synthetic method for preparing 16,17 ketal, particularly to applications of methanesulfonic acid and microwaves in the synthetic method, wherein the reaction speed and the content can be improved.
Synthesis method and application of 9-fluorosteroid compound
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Paragraph 0089-0096; 0137-0139, (2021/01/15)
The invention provides a synthesis method and application of a 9-fluorosteroid compound, and relates to the technical field of chemical synthesis. The synthesis method of the 9-fluorosteroid compoundcomprises the following step: reacting a compound II in an ionic liquid containing hydrogen fluoride salt to obtain a 9-fluorosteroid compound III. According to the synthesis method of the 9-fluorosteroid compound, the ionic liquid containing the hydrogen fluoride salt is used as a fluorinating agent to replace a traditional hydrogen fluoride aqueous solution, volatilization of hydrogen fluoride gas is avoided, corrosivity is small, toxicity is greatly reduced, reaction conditions are mild, reaction can be completed at the room temperature, operability is high, the safety coefficient is high,and production applicability is improved. The synthesis method of the 9-fluorosteroid compound is used for preparing corticosteroid drugs, highly toxic chemical reagents are not used in the synthesisroute, the operability is high, the safety coefficient is high, and the production applicability is improved.
Preparation method of triamcinolone acetonide
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Paragraph 0054-0056, (2018/03/25)
The invention provides a brand new synthesis route for preparation of triamcinolone acetonide; adopted raw materials are cheaper and are easy to obtain, reactive raw materials are hydroxylated and then protection is performed, five-membered ring double bonds are subjected to selective oxidation, a protection group is removed, di-hydroxyl after oxidization is protected, and six-membered ring doublebonds are subjected to epoxidation and then are subjected to ring-opening fluorination to obtain the triamcinolone acetonide product. The reaction process is easy to operate, the yield of each step is relatively high, and the purity of the obtained product is higher, the formation of by-products is effectively avoided, the production cost is reduced and industrialized production is facilitated.
Triamcinolone acetonide acetate preparation method
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Paragraph 0039; 0058; 0059; 0060, (2018/03/24)
The invention provides a full-novel synthesizing route for preparing triamcinolone acetonide acetate. According to the full-novel synthetic route, utilized raw materials have lower cost and more easiness in obtaining. The synthetic route comprises the steps of hydroxylating reaction raw materials and protecting, then selectively oxidizing five-membered ring double bonds, removing a protecting group, then protecting oxidized di-hydroxyl, then epoxidizing six-membered ring double bonds, performing open-ring fluorination and esterfying hydroxyl to obtain a triamcinolone acetonide product. A reaction process has easiness in operation, yields of all the steps are higher, obtained products have higher purities, byproduct generation is effectively avoided, production cost is reduced, and industrial production is facilitated.
Pregnane derivatives 16, 17 - acetal (ketone) preparation method
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Paragraph 0034-0036, (2017/08/31)
Disclosed is a method for preparing a pregnane derivative 16,17-acetal (ketal) compound shown in the general formula I, the method comprising the step of reacting a compound of a general formula II with a compound of a general formula III or a general formula IV in the presence of boron trifluoride, wherein the dotted line between site 1 and site 2 denotes a saturated or unsaturated bond; R is hydroxyl, halogen or -OCOR7, wherein R7 is a C1-C12 linear chain or branched alkyl, a C3-C10 cycloalkyl, a C2-C8 alkenyl or a C2-C8 alkynyl; R1 and R2 are each hydrogen, a C1-C12 linear chain or branched alkyl, a C3-C10 cycloalkyl, a C2-C8 alkenyl or a C2-C8 alkynyl, or R1, R2 and the carbon to which they are connected form a C3-C10 cycloalkyl together, with the provision that R1 and R2 are not hydrogen simultaneously; R3 is hydrogen or -OCOR8, wherein R8 is a C1-C12 linear chain or branched alkyl, or a C3-C10 cycloalkyl; R4 is hydrogen, fluorine or chlorine; R5 is hydrogen, fluorine, chlorine or methyl; and R6 is a C1-C12 linear chain or branched alkyl. Compared with current processes, the method causes little pollution to the environment, has relatively mild reaction conditions, ease of control, reduced energy consumption and low production costs.
Preparation process of triamcinolone acetonide
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, (2017/07/21)
The invention relates to a preparation process of triamcinolone acetonide. The triamcinolone acetonide is prepared by taking an intermediate III as a raw material. The preparation process comprises the following steps of: by taking a hydrofluoric acid-acetone mixed solvent as a solvent, slowly adding the intermediate III in a temperature range of 40 DEG C below zero to 30 DEG C below zero; after adding the raw material, performing a reaction for 4-8 hours; returning the temperature to 5 DEG C below zero to zero DEG C, and continuously performing a reaction for 10-30 min; after reaction, slowly adding the reaction liquid into a potassium carbonate solution; adjusting the PH value to 7.0-7.5; filtering and discharging the material; and drying the same to obtain triamcinolone acetonide. The preparation process shortens the production period, prevents use of a lot of high-matching acetone and is more environmentally friendly.
NOVEL PROCESS FOR PREPARATION OF GLUCOCORTICOID STEROIDS
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, (2016/08/23)
The present invention discloses a process for the preparation of 16, 17-acetals of pregnane derivatives having formula (I) wherein each substituent is independently selected from; R1 is H or CH3; R2 is C1-C6 linear or branched alkyl, alkynyl group or cycloalkyl group; aryl or heteroaryl group; or R1 and R2 combine to form saturated, unsaturated C3-C6 cyclic or heterocyclic ring; R3 and R4 are same or different and each independently represents H or halogen; R5 is -OH or –OCOR wherein R represents H or C1-C6 linear, branched or cyclic alkyl group that may be substituted.
Method for reducing or preventing transplant rejection in the eye and intraocular implants for use therefor
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, (2008/06/13)
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.
