1314705-20-8Relevant articles and documents
Purification method of everolimus
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Paragraph 0087; 0088; 0089, (2019/01/24)
The invention provides a purification method of everolimus. According to the method, derivatization, separation and hydrolysis are carried out on everolimus, the treated everolimus has greatly reducedimpurity rapamycin content, and further by means of one-time preparation of liquid phase for purification, a high purity product with high yield can be obtained, thereby reducing the industrial costof the purification steps. The invention also further provides a preparation method of everolimus. The method has the advantages of high yield and simple operation, and is suitable for industrial production.
Preparation and purification method of everolimus intermediate
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Paragraph 0026; 0027; 0031; 0033; 0039; 0044, (2018/07/03)
The invention discloses a purification method of an everolimus intermediate. The method specifically includes: (1) reacting rapamycin with 2-(tert-butyl diphenylsilyl)oxyethyl trifluoromethanesulfonate to obtain a reaction solution containing an everolimus intermediate shown as formula I; and (2) filtering the everolimus intermediate reaction solution and conducting column chromatography. Specifically, the eluant for column chromatography is successively a small polar organic solvent and a mixed solvent of small polar organic solvent and ethyl acetate, wherein the small polar organic solvent is n-hexane, n-heptane, cyclohexane or methyl tert-butyl ether. After elution by the method of step (2), the mixture of ethyl acetate and small polar organic solvent is adopted as the eluant, and separation is carried out to obtain unreacted rapamycin. The method provided by the invention solves the problems of tedious post-treatment of the everolimus intermediate reaction solution and the need ofcolumn chromatography for petroleum ether.
Pimecrolimus ivermectin intermediate and degrade the impurity of the preparation method
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Paragraph 0033; 0034, (2017/08/25)
The invention discloses methods for preparing everolimus intermediates and everolimus degradation impurities, and particularly relates to methods for synthesizing the immunosuppressant everolimus intermediates and the everolimus degradation impurities rep
METHOD FOR THE SYNTHESIS OF RAPAMYCIN DERIVATIVES
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Page/Page column 14, (2017/01/09)
The present invention relates to a method for the production of a rapamycin derivative of formula (I), the method comprising the preparation of a 2-(tri-substituted silyl)oxyethyl triflate by reacting ethylene oxide and a tri-substituted silyl triflate, reaction of the resulting 2-(tri-substituted silyl)oxyethyl triflate with rapamycin in the presence of a molar excess of organic base, and deprotection to obtain the rapamycin derivative of compound (I).
RAFAMYCIN ANALOGS AND METHODS FOR MAKING SAME
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, (2015/02/25)
A semi-synthetic rapamycin analog with a triazole moiety or a pharmaceutically acceptable salt or prodrug thereof, is a broad-spectrum cytostatic agent and a mTOR inhibitor, and is useful in the treatment of various cancers, or tumors in organs such as kidney, liver, breast, head and neck, lung, prostate, and restenosis in coronary arteries, peripheral arteries, and arteries in the brain, immune and autoimmune diseases. Also disclosed are fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such triazole-moiety containing rapamycin analog is in treating renal carcinoma, lung cancer, colon cancer, and breast cancers wherein potency of the drug, its half-life, tissue distribution properties, and its pharmacokinetic properties including bioavailability through oral and intravenous routes are essential to the clinical outcomes.
ALKYLATION WITH AN ALKYL FLUOROALKYL SULFONATE
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Page/Page column 28; 29, (2015/01/07)
The present invention discloses a process for preparing a chemical compound comprising reacting a nucleophile with an alkyl fluoroalkyi sulfonate in the presence of a base of formula NR1 R2R3, wherein R1 and R2 are independently 2-methylpropyl or isopropyl and R3 is - CH(R4)(R5), wherein R4 and R5 are identical or different alkyls that are optionally connected to form a ring. The invention also relates to a process for preparing an alkyl fluoroalkyi sulfonate. The invention further relates to a use of the base in a chemical reaction comprising an alkyl fluoroalkyi sulfonate. The process and uses are suitable for preparing chemical compounds, reactants or intermediates thereof, and in particular for preparing API or reactants, like for example everolimus or reactants for its preparation.
RAFAMYCIN ANALOGS AND METHODS FOR MAKING SAME
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, (2014/06/23)
A semi-synthetic rapamycin analog with a triazole moiety or a pharmaceutically acceptable salt or prodrug thereof, is a broad-spectrum cytostatic agent and a m TOR inhibitor, and is useful in the treatment of various cancers, or tumors in organs such as kidney, liver, breast, head and neck, lung, prostate, and restenosis in coronary arteries, peripheral arteries, and arteries in the brain, immune and autoimmune diseases. Also disclosed are fungal growth-, restenosis-, post- transplant tissue rejection- and immune- and autoimmune disease- inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal. One particular preferred application of such triazole-moiety containing rapamycin analog is in treating renal carcinoma, lung cancer, colon cancer, and breast cancers wherein potency of the drug, its half-life, tissue distribution properties, and its pharmacokinetic properties including bioavailability through oral and intravenous routes are essential to the clinical outcomes.
