- Synthesis method and application of 9-fluorosteroid compound
-
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.
- -
-
Paragraph 0089-0096; 0131-0133
(2021/01/15)
-
- Preparation method of triamcinolone
-
The invention provides a brand new synthesis route for preparation of triamcinolone; adopted raw materials are cheaper and easier to obtain, reactive raw materials are hydroxylated and then protectionis performed, five-membered ring double bonds are subjected to selective oxidation, generated di-hydroxyl is subjected to esterification protection, then six-membered ring double bonds are subjectedto epoxidation and are subjected to ring-opening fluorination to remove a protective group, and thus the triamcinolone product is obtained. 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.
- -
-
Paragraph 0047-0049
(2018/03/25)
-
- NOVEL PROCESS FOR PREPARATION OF GLUCOCORTICOID STEROIDS
-
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.
- -
-
Page/Page column 26
(2016/08/23)
-
- 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.
- -
-
-
- Mucosal adhesive device for long-acting delivery of pharmaceutical combinations in oral cavity
-
Mucosal adhesive devices are provided for use in the oral cavity for therapy against infections. The devices are dosage units which comprise a combination of antimicrobial agents such as antifungal agents and anti-inflammatory agents, optionally also a local anesthetic. The dosage units yield a gradual and relatively constant release of the pharmaceuticals over at least a 12-hour period.
- -
-
-
- High molecular weight prodrug derivatives of antiinflammatory drugs
-
Compounds of the formula 1, PS - O - A - (CH2)n- B - D (1), wherein PS-O represents an alkoxide residue of any of the free hydroxy groups of a polysaccharide (PS-OH) compound with molecular weight (Mw) of from 40,000 to 5,000,000 selected from dextran, carboxymethyl dextran, diethylaminoethyl dextran, starch, hydroxyet-hyl starch, alginates, glycogen, pullullan, agarose, cellulose, chitosan, chitin and carrageenan,A is a carbonyl group or absent,n is zero or a positive integer from 1 to 14,B is oxygen, a carbonyl group, NR wherein R is hydrogen or lower alkyl, or B is absent, and, D is (i) a group of the formula:, R1 - CO - (11), wherein R1-CO- represents the acyl residue of a carboxylic acid drug (R1-COOH) used in the treatment of inflammatory disorders; or (ii) a group of the formula:, R2 - O - (12), wherein R2-O- refers to the C-21 alkoxide residue of a known antiinflammatory steroid (R2-OH) or an alkoxide residue of any other drug or medicament containing a hydroxy functional group used in the treatment of inflammatory disorders; with the proviso that when A is absent, n is 0, and B is absent, then R1-CO- is different from the acyl residue of acetylsalicylic acid;, and non-toxic pharmaceutically acceptable acid addition salts thereof;, and non-toxic pharmaceutically acceptable cation salts thereof. Such compounds are biolabile prodrugs providing controlled release and prolonged duration of action of the parent active antiinflamma-tory agents locally at the administration site after intra-articular, intra-muscular, subcutaneous or extra-dural application while at the same time being highly stable in aqueous solution in the pH range 3--5. After oral administration of such prodrugs the parent drug is liberated selectively in the terminal ileum and the colon over an extended period of time.
- -
-
-
- Process for preparing salt of hyaluronic acid with a pharmaceutically active substance
-
Pharmaceutical preparations for topical administration containing a pharmacologically active substance together with hyaluronic acid or a molecular weight fraction thereof. The hyaluronic acid may be in the form of the free acid or may be a salt with an alkali or alkaline earth metal, magnesium, aluminum or ammonium, or in the form of a salt with one or more pharmacologically active substances.
- -
-
-
- Amine containing ester prodrugs of corticosteroids
-
Novel solution stable ester prodrugs of corticosteroids of the formula STR1
- -
-
-
- Amine containing ester prodrugs of corticosteroids
-
Novel solution stable ester prodrugs of corticosteroids of the formula STR1
- -
-
-
- Sulfonate containing ester prodrugs of corticosteroids
-
Novel solution stable ester prodrugs of corticosteroids of the formula STR1 and their salts.
- -
-
-
- Sulfonate containing ester prodrugs of corticosteroids
-
Novel solution stable ester prodrugs of corticosteroids of the formula STR1 and their salts.
- -
-
-
- Trimethyl siloxane steroid intermediates
-
A procedure for converting steroids characterized by presence of an 11βOH group into potent corticoids having one or more substituents, such as 6αF, 16α, 17α-hydroxy or isopropylidene dioxy, 16α or 16β methyl, Δ1,4 ; by reacting the 11β-hydroxy steroid with trichloromethyl siloxane steroid, thereby rendering the normally sensitive 11 substituent inert to the series of reactions which thereafter incorporate one or more of the desired above listed substituents into the steroid molecule. The siloxy group is then hydrolyzed to regenerate the 11β-hydroxy substituent. Many of the trimethyl siloxy steroids are novel compounds. The siloxane may be selectively cleaved by reaction of the finely divided steroid with 40-60% aqueous HF.
- -
-
-