- Preparation method of ciclesonide
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The invention discloses a preparation method of ciclesonide. The preparation method comprises the following steps: aldolization reaction, primary purification, hydrolysis reaction, esterification reaction and secondary purification. Aldolization reaction:
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Paragraph 0027-0028; 0032-0035; 0039-0040
(2021/08/07)
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- Ciclesonide preparation method
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The invention discloses a ciclesonide preparation method, and belongs to the technical field of pharmacy, wherein 16[alpha]-hydroxyprednisolone-21-acetate (the previous-step intermediate of 16[alpha]-hydroxyprednisolone) is used as a starting raw material
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Paragraph 0016; 0017; 0021-0023; 0026-0028; 0031; 0032
(2019/02/13)
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- Pregnane derivatives 16, 17 - acetal (ketone) preparation method
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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.
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Paragraph 0043-0045
(2017/08/31)
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- NOVEL PROCESS FOR PREPARATION OF GLUCOCORTICOID STEROIDS
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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.
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- NOVEL METHOD FOR MANUFACTURING OF CICLESONIDE
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The invention relates to a process for preparing ciclesonide in epimerically pure form, a corticosteroid of formula 1: Ciclesonide is used for the treatment of respiratory complaints.
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- NOVEL METHOD FOR MANUFACTURING OF CICLESONIDE
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The invention relates to a process for preparing the corticosteroid ciclesonide, used for the treatment of respiratory complaints, in epimerically pure form of formula 1:
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- Crystalline Ciclesonide Methanol Solvate Form C
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The present invention relates to crystalline ciclesonide methanol solvate Form C, processes for its preparation, its use in the synthesis of crystalline ciclesonide Form A and its use in medicine.
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- PROCESSES FOR THE PREPARATION OF CICLESONIDE AND ITS CRYSTAL MODIFICATION
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Improved processes for the synthesis of ciclesonide, chemically termed as [11β,16α(R)]-16,17-[(cyclohexylmethylene)bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)pregna-1,4-diene-3,20-dione and its crystal modification.
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Page/Page column 4; 7
(2010/09/07)
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- PROCESS FOR THE PREPARATION OF PREGNANE DERIVATIVES
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A stereoselective and enrichment process for the preparation of ciclesonide is described.
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Page/Page column 9
(2009/10/22)
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- Process for the preparation of ciclesonide
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Provided is a process for increasing the 22R/22S epidemic ratio of ciclesonide.
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Page/Page column 3; 4; 5
(2008/06/13)
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- Crystalline forms of ciclesonide
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The invention encompasses a crystalline form of ciclesonide characterized by an XRD pattern having peaks at about 11.0, 14.8, 15.7, 16.5, and 22.8 degrees two-theta±0.2 degrees two-theta, methods of its preparation and pharmaceutical compositions thereof.
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Page/Page column 5
(2008/06/13)
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- One-pot processes for preparing prednisolone derivatives
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Disclosed is a one-pot process for the preparation of a prednisolone derivative of formula I, comprising reacting the compound of formula II with the compound of formula III and the compound of formula IV The process does not need to separate and purify t
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Page/Page column 4
(2008/06/13)
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- CICLESONIDE-CONTAINING AQUEOUS PHARMACEUTICAL COMPOSITION
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The present invention provides an aqueous pharmaceutical composition containing ciclesonide and hydroxypropyl-methylcellulose, wherein the ciclesonide is dispersed in an aqueous medium in the form of solid particles. The composition is able to avoid variations in the concentrations of ciclesonide during production as well as avoid decreases in the recovery rate of ciclesonide.
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