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【结 构 式】

【药物名称】Budesonide, S-1320, Pulmaxan, Pulmicort, Rhinocort, Entocort, Budenofalk, Preferid, Pulmicort turbuhaler, Budiair, Pulmaxan turbohaler, Pulmicort Topinasal, Pulmicort Respules, Inflammide, Giona Easyhaler, Miflonide, Rhinocort Aqua

【化学名称】16alpha,17alpha-(22R,S)-Propylmethylenedioxypregna-1,4-diene-11beta,21-diol-3,20-dione
      (11beta,16alpha)-16,17-[Butylidenebis(oxy)]-11,21-dihydroxypregna-1,4-diene-3,20-dione

【CA登记号】51333-22-3

【 分 子 式 】C25H34O6

【 分 子 量 】430.54613

【开发单位】AstraZeneca (Originator), Boehringer Ingelheim (Not Determined), Teijin (Not Determined), Chiesi (Formulation), CyDex (Formulation), ML Laboratories (Formulation), Orion Corp. (Formulation), Sheffield (Formulation), SkyePharma (Formulation), West Pharmace

【药理作用】Antiallergy/Antiasthmatic Drugs, Asthma Therapy, Drugs for Allergic Rhinitis, GASTROINTESTINAL DRUGS, Inflammatory Bowel Disease, Agents for, RESPIRATORY DRUGS, Treatment of Upper Respiratory Tract Disorders, Corticosteroids

合成路线1

From 16alpha-hydroxyprednisolone (III) and n-butyraldehyde (A) in the presence of an acid catalyst. Budesonide is defined as a 1:1 mixture of the two epimers (I) and (II).

1 Thalen, A.; Brattsand, R.; Synthesis and antiinflammatory properties of budesonide, a new nonhalogenated glucocorticoid with high local activity. Arzneim-Forsch Drug Res 1979, 29, 11, 1687-90.
2 Dharma, A.P.; Budesonide. Drugs Fut 1980, 5, 4, 179.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(A) 23694 butyraldehyde 123-72-8 C4H8O 详情 详情
(III) 32675 (8S,9S,10R,11S,13S,14S,16R,17S)-17-glycoloyl-11,16,17-trihydroxy-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one C21H28O6 详情 详情
Extended Information