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医药中间体

医药中间体是指在药物合成过程中作为关键步骤的反应产物或原料物质,它们通常是化学结构较为简单的化合物,通过一系列化学反应可以转化为最终的药物成品。这些中间体在制药工业中扮演着重要角色,是实现复杂药物分子合成的关键组成部分。

特点
  1. 多样性:医药中间体种类繁多,根据所需药品的不同而不同。
  2. 复杂性:有些医药中间体本身可能较为简单,但通过一系列复杂的化学反应才能获得最终的药物成品。
  3. 安全性与纯度要求高:在制药行业中,医药中间体的安全性和纯度直接影响到最终产品的质量和效果。
应用
  1. 合成新药:许多复杂结构的新药都是通过一些简单的中间体经过一系列复杂的化学反应而合成得到的。
  2. 药物改良:通过对现有药物中的某些关键中间体进行优化,可以开发出更有效的治疗手段或者降低副作用。
  3. 原料供应保障:确保医药中间体的稳定供应对于维持药品市场供给至关重要。
生产与研发

医药中间体的研发和生产是一个复杂的过程,通常包括以下几个步骤:

  • 合成设计:根据目标药物结构设计合适的合成路线。
  • 实验室规模合成与优化:通过小规模实验来验证并优化反应条件。
  • 中试放大:将实验室中的成功方案应用于工业化生产前的中间试验阶段。
  • 工业化生产:在确保安全性和质量的前提下进行大规模生产。
发展趋势

随着化学合成技术的进步和新技术的应用(如绿色化学、计算机辅助设计等),医药中间体的研发与生产正朝着更加高效、环保的方向发展。同时,对药物分子结构的深入理解也为开发更有效的治疗方案提供了更多可能性。

中文名称 英文名称 CAS号 化学式 结构式图片
—— 4-bromo-N-methylpicolinamide 1209459-88-0 C7H7BrN2O
4-bromo-N-methylpicolinamide
—— N-nitroso-ciprofloxacin 864443-44-7 C17H17FN4O4
N-nitroso-ciprofloxacin
—— 8-Methyl-8-azabicyclo[3.2.1]oct-3-yl benzoate 537-26-8 C15H19NO2
8-Methyl-8-azabicyclo[3.2.1]oct-3-yl benzoate
—— O-Desmethyl Quinine 524-63-0 C19H22N2O2
O-Desmethyl Quinine
—— methyl 1-acetyl-3-[ethoxy(phenyl)methylidene]-2-oxo-2,3-dihydro-7H-indole-6-carboxylate 1175365-43-1 C21H19NO5
methyl 1-acetyl-3-[ethoxy(phenyl)methylidene]-2-oxo-2,3-dihydro-7H-indole-6-carboxylate
—— methyl 3-[methoxy(phenyl)methylene]-2-oxoindoline-6-carboxylate 1160293-22-0 C18H15NO4
methyl 3-[methoxy(phenyl)methylene]-2-oxoindoline-6-carboxylate
—— 9α,10β-dehydroprogesterone diethylene ketal 19592-55-3 C25H36O4
9α,10β-dehydroprogesterone diethylene ketal
—— 6α-Hydroxyprogesterone 604-20-6 C21H30O3
6α-Hydroxyprogesterone
—— 2-(4,6-dimethoxy-1,3,5-triazin-2-yl)aminoacetic acid 132786-90-4 C7H10N4O4
2-(4,6-dimethoxy-1,3,5-triazin-2-yl)aminoacetic acid
—— 14-hydroxy-4-pregnene-3,20-dione 16031-66-6 C21H30O3
14-hydroxy-4-pregnene-3,20-dione
—— (S)-5-(tert-butoxy)-4-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)-5-oxopentanoic acid 79640-70-3 C24H30N8O5
(S)-5-(tert-butoxy)-4-(4-(((2,4-diaminopteridin-6-yl)methyl)(methyl)amino)benzamido)-5-oxopentanoic acid
—— 5,6-dihydro-pyran-2-one 3393-45-1 C5H6O2
5,6-dihydro-pyran-2-one
—— tert-butyl (R)-(3-cyclohexenyl)carbamate 1350636-87-1 C11H19NO2
tert-butyl (R)-(3-cyclohexenyl)carbamate
—— 2-biphenyl-4-yl-1-morpholin-4-yl-ethanethione 5428-57-9 C18H19NOS
2-biphenyl-4-yl-1-morpholin-4-yl-ethanethione
—— 2-(hydroxyimino)-6-methoxy-2,3-dihydro-1H-inden-1-one 24077-98-3 C10H9NO3
2-(hydroxyimino)-6-methoxy-2,3-dihydro-1H-inden-1-one
—— (10R,13S,17S)-10,13,17-trimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-3,17-diol 521-10-8 C20H32O2
(10R,13S,17S)-10,13,17-trimethyl-1,2,3,4,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthrene-3,17-diol
—— 1-(4-(tert-butyl)phenyl)-3-(4-hydroxyphenyl)propane-1,3-dione 132944-34-4 C19H20O3
1-(4-(tert-butyl)phenyl)-3-(4-hydroxyphenyl)propane-1,3-dione
—— 3-benzyl-1,2-dimethyl-1H-indole 19006-15-6 C17H17N
3-benzyl-1,2-dimethyl-1H-indole
—— N-Boc-endo-3-aminotropane 207405-68-3 C12H22N2O2
N-Boc-endo-3-aminotropane
—— (1E,3E)-1-chloro-4-(4-phenylbuta-1,3-dien-1-yl)benzene 37985-13-0 C16H13Cl
(1E,3E)-1-chloro-4-(4-phenylbuta-1,3-dien-1-yl)benzene
—— 1-carbamimidoyl-2-methyl-isothiourea hydroiodide 14945-92-7 C3H8N4S*HI
1-carbamimidoyl-2-methyl-isothiourea hydroiodide
—— 2-[(E)-3-phenylprop-2-enyl]-2,3-dihydro-1H-isoindole-1,3-dione 56866-32-1 C17H13NO2
2-[(E)-3-phenylprop-2-enyl]-2,3-dihydro-1H-isoindole-1,3-dione
—— 5-amino-2-hydroxypyridine 33630-94-3 C5H6N2O
5-amino-2-hydroxypyridine
—— N-Boc-nortropinone 185099-67-6 C12H19NO3
N-Boc-nortropinone
—— Samidorphan 852626-89-2 C21H26N2O4
Samidorphan
—— 3-Carboxamidonaltrexone 421552-35-4 C21H24N2O4
3-Carboxamidonaltrexone
—— 6,6-dimethyldihydro-2H-pyran-2,4(3H)-dione 84465-82-7 C7H10O3
6,6-dimethyldihydro-2H-pyran-2,4(3H)-dione
—— N<sup>2</sup>-isobutyryl-2',3'-didehydro-2',3'-dideoxyguanosine 119794-40-0 C14H17N5O4
N<sup>2</sup>-isobutyryl-2',3'-didehydro-2',3'-dideoxyguanosine
—— 9-(β-D-ribofuranosyl)-2,6-diamino-8-bromopurine 81102-44-5 C10H13BrN6O4
9-(β-D-ribofuranosyl)-2,6-diamino-8-bromopurine
—— N<sup>2</sup>-isobutyryl-2',3'-dideoxyguanosine 85326-13-2 C14H19N5O4
N<sup>2</sup>-isobutyryl-2',3'-dideoxyguanosine
—— cupreine 524-63-0 C19H22N2O2
cupreine
—— L-mannonic acid 133-42-6 C6H12O7
L-mannonic acid
—— 16-α hydroxyprednisonlone acetate 86401-80-1 C23H30O7
16-α hydroxyprednisonlone acetate
—— 3,4-dihydro-6-(3-methoxyphenyl)-2-methylthio-4-oxopyrimidine-5-carbonitrile 128640-73-3 C13H11N3O2S
3,4-dihydro-6-(3-methoxyphenyl)-2-methylthio-4-oxopyrimidine-5-carbonitrile
—— 1,6-anhydro-2-azido-2-deoxy-β-D-glucopyranose 67546-20-7 C6H9N3O4
1,6-anhydro-2-azido-2-deoxy-β-D-glucopyranose
—— sodium nicotinate 54-86-4 C6H4NO2*Na
sodium nicotinate
—— Vitamin K1 2,3-epoxide 25486-55-9 C31H46O3
Vitamin K1 2,3-epoxide
—— trans-1,2-dithiane-4,5-diol 14193-38-5 C4H8O2S2
trans-1,2-dithiane-4,5-diol
—— 3-cyclobutyl-1H-pyrazole 476629-86-4 C7H10N2
3-cyclobutyl-1H-pyrazole
—— 2-(4-oxo-3-((5-(trifluoromethyl)benzo[d]thiazol-2-yl)methyl)-3,4-dihydrothieno[3,4-d]pyridazin-1-yl)acetic acid 2170729-29-8 C17H10F3N3O3S2
2-(4-oxo-3-((5-(trifluoromethyl)benzo[d]thiazol-2-yl)methyl)-3,4-dihydrothieno[3,4-d]pyridazin-1-yl)acetic acid
—— allo-inositol 643-10-7 C6H12O6
allo-inositol
—— ethyl 4,7-difluoro-1H-indole-2-carboxylate 394223-44-0 C11H9F2NO2
ethyl 4,7-difluoro-1H-indole-2-carboxylate
—— N-benzylcinchoninium chloride 69221-14-3 C26H29N2O*Cl
N-benzylcinchoninium chloride
—— (1S,9S)-t-butyl octahydro-10-oxo-9-phthalimido-6H-pyridazino<1,2-a><1,2>diazepine-1-carboxylate 106927-97-3 C22H27N3O5
(1S,9S)-t-butyl octahydro-10-oxo-9-phthalimido-6H-pyridazino<1,2-a><1,2>diazepine-1-carboxylate
—— 2-chloro-4-[2-naphthyl]pyrimidine 488816-96-2 C14H9ClN2
2-chloro-4-[2-naphthyl]pyrimidine
—— farnesyl bromide 28290-41-7 C15H25Br
farnesyl bromide
—— 2-deoxy-3,5-di-O-p-chlorobenzoyl-L-chlororibose 21740-23-8 C19H15Cl3O5
2-deoxy-3,5-di-O-p-chlorobenzoyl-L-chlororibose
—— (2R,4R)-1-tert-butyl 2-(2-(9-((2S,5S)-1-((S)-2-(methoxycarbonylamino)-3-methylbutanoyl)-5-methylpyrrolidine-2-carbonyloxy)-8-oxo-8,9,10,11-tetrahydro-5H-dibenzo[c,g]chromen-3-yl)-2-oxoethyl) 4-(methoxymethyl)pyrrolidine-1,2-dicarboxylate 1378391-43-5 C44H55N3O13
(2R,4R)-1-tert-butyl 2-(2-(9-((2S,5S)-1-((S)-2-(methoxycarbonylamino)-3-methylbutanoyl)-5-methylpyrrolidine-2-carbonyloxy)-8-oxo-8,9,10,11-tetrahydro-5H-dibenzo[c,g]chromen-3-yl)-2-oxoethyl) 4-(methoxymethyl)pyrrolidine-1,2-dicarboxylate
—— (2S,4S)-2-(2-(9-bromo-8-oxo-8,9,10,11-tetrahydro-5H-dibenzo[c,g]chromen-3-yl)-2-oxoethyl) 1-tert-butyl 4-(methoxymethyl)pyrrolidine-1,2-dicarboxylate 1378391-42-4 C31H34BrNO8
(2S,4S)-2-(2-(9-bromo-8-oxo-8,9,10,11-tetrahydro-5H-dibenzo[c,g]chromen-3-yl)-2-oxoethyl) 1-tert-butyl 4-(methoxymethyl)pyrrolidine-1,2-dicarboxylate
—— 5,5'-dibromo-8,8'-biquinoline 1148152-49-1 C18H10Br2N2
5,5'-dibromo-8,8'-biquinoline