- 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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- 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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- 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 0040-0042
(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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- STEROID COMPOUND
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A steroid compound of the Formula (1): [wherein R1 represents a group selected from the group consisting of H, CH3, C2H5, C3H7 and CH (CH3)2, R2 represents a group selected from NH2, NHAc and OCOR1, R3 represents a group selected from the group consisting of CH3, COOCH3 and CH2OCOR1.]
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Page/Page column 5
(2012/02/04)
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- STEROID COMPOUND
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A steroid compound of the Formula (1): [wherein R1 represents a group selected from the group consisting of H, CH3, C2H5, C3H7 and CH (CH3)2, R2 represents a group selected from NH2, NHAc and OCOR1, R3 represents a group selected from the group consisting of CH3, COOCH3 and CH2OCOR1.]
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Page/Page column 3
(2012/03/26)
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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 5; 8
(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 8; 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 5
(2008/06/13)
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- SUBSTITUTED PHENYLPHOSPHATES AS MUTUAL PRODRUGS OF STEROIDS AND β -AGONISTS FOR THE TREATMENT OF PULMONARY INFLAMMATION AND BRONCHOCONSTRICTION
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A mutual prodrug of a corticosteroid and a substituted phenylphosphate (β-agonist derivative) for formulation for delivery by aerosolization to inhibit pulmonary inflammation and bronchoconstriction is described. The mutual prodrug is preferably formulate
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Page/Page column 42-43
(2008/06/13)
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- BENZYLPHOSPHATE AND SUBSTITUTED BENZYLPHOSPHATE PRODRUGS FOR TRE TREATMENT OF PULMONARY INFLAMMATION
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A prodrug of a corticosteroid, lidocaine or related local anesthetic composition for formulation for delivery by aerosolization to inhibit inflammation in asthmatic lungs is described. The prodrug is preferably formulated in a 5 ml solution of a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract inflammation by an aerosol having mass medium average diameter predominantly between 1 to 5 μ produced by nebulization or dry powder inhaler.
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Page/Page column 18; 49
(2010/02/12)
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