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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-butyl-4-chloro-1-{[2'-(2-trityl-2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid 960231-60-1 C41H35ClN6O2
2-butyl-4-chloro-1-{[2'-(2-trityl-2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazole-5-carboxylic acid
—— 6-(2-methyl-2-propenyl)imidazo<1,2-a>pyridine 116355-20-5 C11H12N2
6-(2-methyl-2-propenyl)imidazo<1,2-a>pyridine
—— 6-Methylen-4-androsten-3,17-dion 19457-55-7 C20H26O2
6-Methylen-4-androsten-3,17-dion
—— 2,5-dimethoxy-β-nitrostyrene 40276-11-7 C10H11NO4
2,5-dimethoxy-β-nitrostyrene
—— difelikefalin 1024828-77-0 C36H53N7O6
difelikefalin
—— adenosine 5'-diphosphate sodium salt 20398-34-9 C10H14N5O10P2*Na
adenosine 5'-diphosphate sodium salt
—— N-(3,4-dimethoxyphenethyl)cinnamamide 29946-61-0 C19H21NO3
N-(3,4-dimethoxyphenethyl)cinnamamide
—— 2-methyl-3-benzylindole 19006-14-5 C16H15N
2-methyl-3-benzylindole
—— 4-((R)-2-{[6-((S)-3-methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic acid butyl ester 1159500-34-1 C28H39N6O8P
4-((R)-2-{[6-((S)-3-methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic acid butyl ester
—— (+)-Tranylcypromine hydrochloride 4548-34-9 C9H11N*ClH
(+)-Tranylcypromine hydrochloride
—— 1-(p-bromophenacyl)pyridinium bromide 17282-37-0 Br*C13H11BrNO
1-(p-bromophenacyl)pyridinium bromide
—— 8-methyl-3,8-diazabicyclo(3.2.1)octane dihydrochloride 17783-50-5 C7H14N2*2ClH
8-methyl-3,8-diazabicyclo(3.2.1)octane dihydrochloride
—— 4'-(methoxycarbonyl)-[2,2'-bipyridine]-4-carboxylic acid 161955-60-8 C13H10N2O4
4'-(methoxycarbonyl)-[2,2'-bipyridine]-4-carboxylic acid
—— {[3,3-dibutyl-7-(methylsulfanyl)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetic acid 439088-13-8 C26H35NO5S2
{[3,3-dibutyl-7-(methylsulfanyl)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetic acid
—— 5,6-dimethoxy-2-methoxycarbonylindan-1-one 119035-03-9 C13H14O5
5,6-dimethoxy-2-methoxycarbonylindan-1-one
—— 2-cyclopentyl-6-methoxyisonicotinic acid 1122089-67-1 C12H15NO3
2-cyclopentyl-6-methoxyisonicotinic acid
—— tert-butyl 3-(piperidin-3-yl)azetidine-1-carboxylate 1251006-73-1 C13H24N2O2
tert-butyl 3-(piperidin-3-yl)azetidine-1-carboxylate
—— 2,5-bis(4-pyridyl)thiazolo[5,4-d]thiazole 97193-46-9 C14H8N4S2
2,5-bis(4-pyridyl)thiazolo[5,4-d]thiazole
—— Lys-MCC-MDC 1281816-04-3 C53H75ClN6O15S
Lys-MCC-MDC
—— trans-maxacalcitol 103909-75-7 C26H42O4
trans-maxacalcitol
—— 5,5'-(9,10-Dihydrophenanthrene-2,7-diyl)diisophthalic acid 1173286-48-0 C30H20O8
5,5'-(9,10-Dihydrophenanthrene-2,7-diyl)diisophthalic acid
—— 5-bromo-3-phenyl-1H-indole 54470-19-8 C14H10BrN
5-bromo-3-phenyl-1H-indole
—— N-[(S)-(2,3,4,5,6-Pentafluorophenoxy)Phenoxyphosphinyl]-L-Alanine 1-Methylethyl Ester 1334513-02-8 C18H17F5NO5P
N-[(S)-(2,3,4,5,6-Pentafluorophenoxy)Phenoxyphosphinyl]-L-Alanine 1-Methylethyl Ester
—— 5-(2-(4-fluoro-3-methoxy-5-methylphenylamino)-5-methylpyrimidin-4-ylamino)benzo[d]oxazol-2(3H)-one 1236667-40-5 C20H18FN5O3
5-(2-(4-fluoro-3-methoxy-5-methylphenylamino)-5-methylpyrimidin-4-ylamino)benzo[d]oxazol-2(3H)-one
—— SMDPPEH 1093468-95-1 C58H72N2O2S6
SMDPPEH
—— GDC-9545 1953133-47-5 C27H31F5N4O
GDC-9545
—— (1E,5R)-3-Phenylmethyl-4-thia-2,6-diazabicyclo[3.2.0]hept-2-en-7-one 34103-69-0 C11H10N2OS
(1E,5R)-3-Phenylmethyl-4-thia-2,6-diazabicyclo[3.2.0]hept-2-en-7-one
—— (1-Brom-cyclopentyl)-phenyl-keton 6740-66-5 C12H13BrO
(1-Brom-cyclopentyl)-phenyl-keton
—— diethyl 8-hydroxy-2,2,14,14-tetramethylpentadecanedioate 738606-64-9 C23H44O5
diethyl 8-hydroxy-2,2,14,14-tetramethylpentadecanedioate
—— 3-hydroxy-3-methylbutyryl-CoA 6711-29-1 C26H44N7O18P3S
3-hydroxy-3-methylbutyryl-CoA
—— 4-bromo-1-chloro-2-(4-(2-cyclopropoxyethoxy)benzyl)benzene 1118567-45-5 C18H18BrClO2
4-bromo-1-chloro-2-(4-(2-cyclopropoxyethoxy)benzyl)benzene
—— N<sup>6</sup>-(4-fluorobenzyl)pyridine-2,3,6-triamine 112523-78-1 C12H13FN4
N<sup>6</sup>-(4-fluorobenzyl)pyridine-2,3,6-triamine
—— 1,7-dichloroisoquinolin-4-ol 1028252-14-3 C9H5Cl2NO
1,7-dichloroisoquinolin-4-ol
—— 5,6-dimethoxy-2-[(pyridin-4-yl)methylene]-1-indanone 4803-74-1 C17H15NO3
5,6-dimethoxy-2-[(pyridin-4-yl)methylene]-1-indanone
—— N-formyl-1-bromo-narwedine 122584-14-9 C17H16BrNO4
N-formyl-1-bromo-narwedine
—— sodium gentisate 4955-90-2 C7H5O4*Na
sodium gentisate
—— 3-(5-nitrofurfurylideneamino)hydantoic acid 63981-22-6 C8H8N4O6
3-(5-nitrofurfurylideneamino)hydantoic acid
—— 4-(4-Chlorophenyl)Cyclohexanecarboxylic Acid 95233-37-7 C13H15ClO2
4-(4-Chlorophenyl)Cyclohexanecarboxylic Acid
—— (3R,4S,5S,6R,7R,9R,11S,12R,13S,14R)-6-[(3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-10-hydroxyimino-4-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one 13127-18-9 C37H68N2O13
(3R,4S,5S,6R,7R,9R,11S,12R,13S,14R)-6-[(3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-10-hydroxyimino-4-[(4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one
—— 4-[(R)-[(2S,4S,5S)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-hydroxymethyl]quinolin-6-ol 524-63-0 C19H22N2O2
4-[(R)-[(2S,4S,5S)-5-ethenyl-1-azabicyclo[2.2.2]octan-2-yl]-hydroxymethyl]quinolin-6-ol
—— 2-(4-nitro-phenyl)-butyric acid 7463-53-8 C10H11NO4
2-(4-nitro-phenyl)-butyric acid
—— tert-butyl (R)-3-(hydrazinecarbonyl)pyrrolidine-1-carboxylate 1407997-80-1 C10H19N3O3
tert-butyl (R)-3-(hydrazinecarbonyl)pyrrolidine-1-carboxylate
—— (1S,2S,3S,5S)-5-[2-[[(4-methoxyphenyl)diphenylmethyl]amino]-6-benzyloxy-9H-purin-9-yl]-3-benzyloxy-2-[(benzyloxy)methyl]cyclopentanol 142217-78-5 C52H49N5O5
(1S,2S,3S,5S)-5-[2-[[(4-methoxyphenyl)diphenylmethyl]amino]-6-benzyloxy-9H-purin-9-yl]-3-benzyloxy-2-[(benzyloxy)methyl]cyclopentanol
—— 18-epi-β-amyrin 559-70-6 C30H50O
18-epi-β-amyrin
—— (E)-1,3-dimethoxy-2-(1-methylethyl)-5-(2-phenylethenyl)benzene 141509-20-8 C19H22O2
(E)-1,3-dimethoxy-2-(1-methylethyl)-5-(2-phenylethenyl)benzene
—— (S)-3-methylindoline 291540-52-8 C9H11N
(S)-3-methylindoline
—— 10,11-Dihydro-10-(2-chloro-4-aminobenzoyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine 168079-19-4 C19H16ClN3O
10,11-Dihydro-10-(2-chloro-4-aminobenzoyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepine
—— (2-chloro-4-nitrophenyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-yl-methanone 179063-21-9 C19H14ClN3O3
(2-chloro-4-nitrophenyl)-5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-yl-methanone
—— <5-<sup>2</sup>H>uracil 24897-50-5 C4H4N2O2
<5-<sup>2</sup>H>uracil
—— #rac-Ergolin-8β-carbonsaeure-methylester 30341-92-5 C16H18N2O2
#rac-Ergolin-8β-carbonsaeure-methylester