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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
—— 2-Fluoro-9-(2,3,5-tri-o-acetylpentofuranosyl)-9h-purin-6-amine 15811-32-2 C16H18FN5O7
2-Fluoro-9-(2,3,5-tri-o-acetylpentofuranosyl)-9h-purin-6-amine
—— (±)-2-(methylaminomethyl)-3,4-dihydro-2H-naphthalen-1-one 403860-66-2 C12H15NO
(±)-2-(methylaminomethyl)-3,4-dihydro-2H-naphthalen-1-one
—— 1,2:3,4-Di-O-isopropylidene-6-deoxy-6-tosyl-alpha-D-galactopyranose 4478-43-7 C19H26O8S
1,2:3,4-Di-O-isopropylidene-6-deoxy-6-tosyl-alpha-D-galactopyranose
—— 6-amino-2-mercapto-3H-pyrimidin-4-one monohydrate 65802-56-4 C4H7N3O2S
6-amino-2-mercapto-3H-pyrimidin-4-one monohydrate
—— 3,5-Bis-o-(4-chlorobenzoyl)-2-deoxypentofuranosyl chloride 21740-23-8 C19H15Cl3O5
3,5-Bis-o-(4-chlorobenzoyl)-2-deoxypentofuranosyl chloride
—— 4,8-dihidrobenzo<1,2-c:4,5-c'>dithiophene-4,8-dione 33527-23-0 C10H4O2S2
4,8-dihidrobenzo<1,2-c:4,5-c'>dithiophene-4,8-dione
—— 3,3-dimethyltetrahydro-2H-pyran-4-amine 1357396-54-3 C7H15NO
3,3-dimethyltetrahydro-2H-pyran-4-amine
—— 1-(4-carboxyphenyl)-3-methyl-5-pyrazolone 60875-16-3 C11H10N2O3
1-(4-carboxyphenyl)-3-methyl-5-pyrazolone
—— 4-Amino-8-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-oxopyrido[2,3-d]pyrimidine-6-carboxamide 36707-00-3 C13H15N5O6
4-Amino-8-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-oxopyrido[2,3-d]pyrimidine-6-carboxamide
—— (1S,3R,4R,6S,7S)-3-(6-N-benzoyladenin-9-yl)-7-[2-cyanoethoxy(diisopropylamino)phosphinoxy]-1-(4,4'-dimethoxytrityloxymethyl)-6-methyl-2,5-dioxabicyclo[2.2.1]heptane 1197033-19-4 C49H54N7O8P
(1S,3R,4R,6S,7S)-3-(6-N-benzoyladenin-9-yl)-7-[2-cyanoethoxy(diisopropylamino)phosphinoxy]-1-(4,4'-dimethoxytrityloxymethyl)-6-methyl-2,5-dioxabicyclo[2.2.1]heptane
—— (1S,3R,4R,6S,7S)-7-[2-cyanoethoxy(diisopropylamino)phosphinoxy]-1-(4,4'-dimethoxytrityloxymethyl)-6-methyl-3-(thymin-1-yl)-2,5-dioxabicyclo[2.2.1]heptane 1197033-22-9 C42H51N4O9P
(1S,3R,4R,6S,7S)-7-[2-cyanoethoxy(diisopropylamino)phosphinoxy]-1-(4,4'-dimethoxytrityloxymethyl)-6-methyl-3-(thymin-1-yl)-2,5-dioxabicyclo[2.2.1]heptane
—— tert-butyl ((3R,6R)-6-methylpiperidin-3-yl)carbamate 1222491-53-3 C11H22N2O2
tert-butyl ((3R,6R)-6-methylpiperidin-3-yl)carbamate
—— (+/-)-(Z)-methyl 4-(2-amino-5-(4-((dimethylamino)methyl)thiophen-2-yl)pyridin-3-yl)-2-((5,5,5-trifluoropent-3-en-2-yl)oxy)benzoate 1364268-07-4 C25H26F3N3O3S
(+/-)-(Z)-methyl 4-(2-amino-5-(4-((dimethylamino)methyl)thiophen-2-yl)pyridin-3-yl)-2-((5,5,5-trifluoropent-3-en-2-yl)oxy)benzoate
—— 3-amino-4-isopropylpyridine 1337991-84-0 C8H12N2
3-amino-4-isopropylpyridine
—— (-)-methyl (1S,2S,3R,4R)-3-[(1S)-1-(acetylamino)-2-ethylbutyl]-4-amino-2-hydroxycyclopentanecarboxylate 229615-05-8 C15H28N2O4
(-)-methyl (1S,2S,3R,4R)-3-[(1S)-1-(acetylamino)-2-ethylbutyl]-4-amino-2-hydroxycyclopentanecarboxylate
—— 2,3,4,6-tetra-O-benzyl-1-C-(dichloromethyl)-D-glucopyranose 140658-50-0 C35H36Cl2O6
2,3,4,6-tetra-O-benzyl-1-C-(dichloromethyl)-D-glucopyranose
—— ((S)-pyrrolidin-2-yl)acetonitrile hydrochloride 1413085-67-2 C6H10N2*ClH
((S)-pyrrolidin-2-yl)acetonitrile hydrochloride
—— 6-chloro-8-methyl-imidazo[1,2-<i>b</i>]pyridazine-2-carboxylic acid 64068-13-9 C8H6ClN3O2
6-chloro-8-methyl-imidazo[1,2-<i>b</i>]pyridazine-2-carboxylic acid
—— ethyl 4-oxo-1H-1,10-phenanthroline-3-carboxylate 49590-04-7 C15H12N2O3
ethyl 4-oxo-1H-1,10-phenanthroline-3-carboxylate
—— (3R,4R)-4-amino-3-methyl-piperidine-1-carboxylic acid tert-butyl ester 723308-58-5 C11H22N2O2
(3R,4R)-4-amino-3-methyl-piperidine-1-carboxylic acid tert-butyl ester
—— 5-anilino-2-hydroxy-penta-2,4-dienal-phenylimine; hydrochloride 17315-76-3 C17H16N2O*ClH
5-anilino-2-hydroxy-penta-2,4-dienal-phenylimine; hydrochloride
—— 4-Amino-1-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methoxypyrimidin-2-one 37805-90-6 C10H15N3O6
4-Amino-1-[3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methoxypyrimidin-2-one
—— 1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid ethyl ester 1499823-71-0 C11H16N2O3
1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-carboxylic acid ethyl ester
—— ethyl 6-chloro-8-methylimidazo[1,2-b]pyridazine-2-carboxylate 64068-04-8 C10H10ClN3O2
ethyl 6-chloro-8-methylimidazo[1,2-b]pyridazine-2-carboxylate
—— 2'-Chlor-2'-desoxy-Ψ-uridin 4753-04-2 C9H11ClN2O5
2'-Chlor-2'-desoxy-Ψ-uridin
—— (S)-methyl-N-(1-phenylethyl)-2-azabicyclo[2.2.1]hept-5-ene-3-carboxylate 130194-96-6 C16H19NO2
(S)-methyl-N-(1-phenylethyl)-2-azabicyclo[2.2.1]hept-5-ene-3-carboxylate
—— FGI-106 free base 501081-38-5 C28H38N6
FGI-106 free base
—— Ethyl 3-(quinolin-4-YL)prop-2-enoate 69976-10-9 C14H13NO2
Ethyl 3-(quinolin-4-YL)prop-2-enoate
—— 3-quinolin-4-yl-acrylic acid ethyl ester 448952-61-2 C14H13NO2
3-quinolin-4-yl-acrylic acid ethyl ester
—— Hexahydro-3-phenyl-5H-oxazolo[3,2-a]pyridine-5-carbonitrile 402846-46-2 C14H16N2O
Hexahydro-3-phenyl-5H-oxazolo[3,2-a]pyridine-5-carbonitrile
—— (2R,3S,4R,5R,6S)-5-amino-6-[(2R,4R,5R)-5-amino-6-[(2R,3S,4R,5R,6R)-5-amino-4,6-dihydroxy-2-(hydroxymethyl)oxan-3-yl]oxy-4-hydroxy-2-(hydroxymethyl)oxan-3-yl]oxy-2-(hydroxymethyl)oxane-3,4-diol 78341-33-0 C18H35N3O13
(2R,3S,4R,5R,6S)-5-amino-6-[(2R,4R,5R)-5-amino-6-[(2R,3S,4R,5R,6R)-5-amino-4,6-dihydroxy-2-(hydroxymethyl)oxan-3-yl]oxy-4-hydroxy-2-(hydroxymethyl)oxan-3-yl]oxy-2-(hydroxymethyl)oxane-3,4-diol
—— 4-[(R)-[(2S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-hydroxymethyl]quinolin-6-ol 524-63-0 C19H22N2O2
4-[(R)-[(2S,5R)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-hydroxymethyl]quinolin-6-ol
—— (+)-1-phenyl-1-[2]pyridyl-ethanol 19490-92-7 C13H13NO
(+)-1-phenyl-1-[2]pyridyl-ethanol
—— 2-(3-isopropylphenyl)pyridine 1314921-39-5 C14H15N
2-(3-isopropylphenyl)pyridine
—— (3R,6R)-6-[(1R,3aS,7aR)-4-[2-[(5S)-5-hydroxy-2-methylenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]-2-methylheptane-2,3-diol 55721-11-4 C27H44O3
(3R,6R)-6-[(1R,3aS,7aR)-4-[2-[(5S)-5-hydroxy-2-methylenecyclohexylidene]ethylidene]-7a-methyl-2,3,3a,5,6,7-hexahydro-1H-inden-1-yl]-2-methylheptane-2,3-diol
—— 2',3'-dideoxy-N6-benzoyl-adenosine 77244-86-1 C17H17N5O3
2',3'-dideoxy-N6-benzoyl-adenosine
—— ethyl 5-oxo-2H-1,2-oxazole-3-carboxylate 88393-81-1 C6H7NO4
ethyl 5-oxo-2H-1,2-oxazole-3-carboxylate
—— 3-Amino-6-(chloromethyl)-2-pyrazinecarbonitrile 4-oxide 40127-89-7 C6H5ClN4O
3-Amino-6-(chloromethyl)-2-pyrazinecarbonitrile 4-oxide
—— 6-Chlor-4-amino-chinolin 103028-97-3 C9H7ClN2
6-Chlor-4-amino-chinolin
—— Pyridine, 2-[2-(dibutylphosphino)ethyl]- 120517-35-3 C15H26NP
Pyridine, 2-[2-(dibutylphosphino)ethyl]-
—— Clicoemodin 34298-85-6 C21H20O10
Clicoemodin
—— 4-[(S)-[(2R,4R,5S)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-hydroxymethyl]quinolin-6-ol 524-63-0 C19H22N2O2
4-[(S)-[(2R,4R,5S)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-hydroxymethyl]quinolin-6-ol
—— (4-bromo-2-fluorophenyl)(3,4,5-trimethoxyphenyl)methanone 1016544-26-5 C16H14BrFO4
(4-bromo-2-fluorophenyl)(3,4,5-trimethoxyphenyl)methanone
—— 6-(α-Styryl)pyridazin-3(2H)-one 83516-65-8 C12H10N2O
6-(α-Styryl)pyridazin-3(2H)-one
—— cis-1-Methyl-2-<2-(2-thienyl)vinyl)>-Δ<sup>2</sup>-tetrahydropyrimidin-tartrat 21573-92-2 C4H6O6*C11H14N2S
cis-1-Methyl-2-<2-(2-thienyl)vinyl)>-Δ<sup>2</sup>-tetrahydropyrimidin-tartrat
—— 5-cyano-4-chloro-6-phenylpyrimidine 40889-24-5 C11H6ClN3
5-cyano-4-chloro-6-phenylpyrimidine
—— N-(p-methoxybenzyl)azepane-2,4-dione 910248-54-3 C14H17NO3
N-(p-methoxybenzyl)azepane-2,4-dione
—— (5R)-1-benzyl-5-ethoxyimidazolidine-2,4-dione 65855-02-9 C12H14N2O3
(5R)-1-benzyl-5-ethoxyimidazolidine-2,4-dione
—— 4-oxaspiro[2.5]octan-7-one 1359869-22-9 C7H10O2
4-oxaspiro[2.5]octan-7-one
—— 1-methyl-2-oxo-2,3-dihydro-1H-indole-6-carbonitrile 1255957-68-6 C10H8N2O
1-methyl-2-oxo-2,3-dihydro-1H-indole-6-carbonitrile