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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
—— (2Z)-3-(thiophen-2-yl)prop-2-enenitrile 6041-28-7 C7H5NS
(2Z)-3-(thiophen-2-yl)prop-2-enenitrile
—— (2E)-3-(thiophen-2-yl)prop-2-enenitrile 6041-28-7 C7H5NS
(2E)-3-(thiophen-2-yl)prop-2-enenitrile
—— (4R,6S)-2,4,6-trimethyl-1,3,5-dithiazinane 638-17-5 C6H13NS2
(4R,6S)-2,4,6-trimethyl-1,3,5-dithiazinane
—— N,N'-Dicarbobenzoxy-L-β-lysin 35107-12-1 C22H26N2O6
N,N'-Dicarbobenzoxy-L-β-lysin
—— 2,4-quinolinediol monosodium salt 4510-76-3 C9H6NO2*Na
2,4-quinolinediol monosodium salt
—— (S)-[(2R)-1-benzyl-5-ethenyl-1-azoniabicyclo[2.2.2]octan-2-yl]-quinolin-4-ylmethanol;chloride 69221-14-3 C26H29ClN2O
(S)-[(2R)-1-benzyl-5-ethenyl-1-azoniabicyclo[2.2.2]octan-2-yl]-quinolin-4-ylmethanol;chloride
—— (1-Benzyl-5-ethenyl-1-azoniabicyclo[2.2.2]octan-2-yl)-quinolin-4-ylmethanol;chloride 69257-04-1 C26H29ClN2O
(1-Benzyl-5-ethenyl-1-azoniabicyclo[2.2.2]octan-2-yl)-quinolin-4-ylmethanol;chloride
—— Penicillin V sulfoxid 4888-90-8 C16H18N2O6S
Penicillin V sulfoxid
—— 2'-O-[2-(methylamino)-2-oxoethyl]-5-methyluridine 815632-50-9 C13H19N3O7
2'-O-[2-(methylamino)-2-oxoethyl]-5-methyluridine
—— 2-aminocyclohexanecarboxamide 34126-95-9 C7H14N2O
2-aminocyclohexanecarboxamide
—— (2S,4S)-N-Boc-4-hydroxypiperidine-2-carboxylic acid 441044-12-8 C11H19NO5
(2S,4S)-N-Boc-4-hydroxypiperidine-2-carboxylic acid
—— 7-amino-3-hydroxycepham-4-carboxylic acid 68403-70-3 C7H10N2O4S
7-amino-3-hydroxycepham-4-carboxylic acid
—— 7-chloro-3-iodoimidazo[1,2-a]pyridine 908267-60-7 C7H4ClIN2
7-chloro-3-iodoimidazo[1,2-a]pyridine
—— 3-chlorodibenzothiophene 109014-35-9 C12H7ClS
3-chlorodibenzothiophene
—— 2-hydroxy-6-bromobenzopyridin-4-one 138964-51-9 C9H6BrNO2
2-hydroxy-6-bromobenzopyridin-4-one
—— 5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide hydrochloride 1426309-48-9 C14H11F2N5*ClH
5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carboximidamide hydrochloride
—— (Z,2R)-5-amino-2-(dibenzylamino)-1,6-diphenylhex-4-en-3-one 156732-13-7 C32H32N2O
(Z,2R)-5-amino-2-(dibenzylamino)-1,6-diphenylhex-4-en-3-one
—— 3-<(tert-Butoxycarbonyl)amino>-4-hydroxy-L-butyric acid 83345-44-2 C9H17NO5
3-<(tert-Butoxycarbonyl)amino>-4-hydroxy-L-butyric acid
—— (Z)-2-(hydroxyimino)-6-methoxy-2,3-dihydro-1H-inden-1-one 24077-98-3 C10H9NO3
(Z)-2-(hydroxyimino)-6-methoxy-2,3-dihydro-1H-inden-1-one
—— 5-(trifluoromethyl)-1H-pyrimidine-2,4-di(17O2)one 54-20-6 C5H3F3N2O2
5-(trifluoromethyl)-1H-pyrimidine-2,4-di(17O2)one
—— (S)-(-)-Blebbistatin O-Benzoate 1217832-61-5 C25H20N2O3
(S)-(-)-Blebbistatin O-Benzoate
—— (S,E)-4,8-dimethylnona-3,7-dien-2-ol 67845-50-5 C11H20O
(S,E)-4,8-dimethylnona-3,7-dien-2-ol
—— (4R,5R)-4,5-dimethyl-1,3,2-dioxathiolane 2,2-dioxide 106757-36-2 C4H8O4S
(4R,5R)-4,5-dimethyl-1,3,2-dioxathiolane 2,2-dioxide
—— ellipticine quinone 73326-98-4 C15H8N2O2
ellipticine quinone
—— 5-bromo-4-methyl-8-hydropyrazolo[1,5-a]pyridine 1345121-43-8 C8H7BrN2
5-bromo-4-methyl-8-hydropyrazolo[1,5-a]pyridine
—— 4-bromo-5-methyl-pyrazolo[1,5-a]pyridine 1345121-29-0 C8H7BrN2
4-bromo-5-methyl-pyrazolo[1,5-a]pyridine
—— (S)-α-methylserine hydrochloride 114396-62-2 C4H9NO3*ClH
(S)-α-methylserine hydrochloride
—— 4'-(bromomethyl)-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide 1026273-26-6 C23H27BrN2O5S
4'-(bromomethyl)-N-(4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide
—— 4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl-N-](4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide 1026355-73-6 C34H44N4O6S
4'-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl-N-](4,5-dimethyl-3-isoxazolyl)-2'-(ethoxymethyl)-N-(methoxymethyl) [1,1'-biphenyl]-2-sulfonamide
—— tert-butyl (3S)-3-[methoxy(methyl)carbamoyl]pyrrolidine-1-carboxylate 1204677-53-1 C12H22N2O4
tert-butyl (3S)-3-[methoxy(methyl)carbamoyl]pyrrolidine-1-carboxylate
—— 3-hydroxy-5-methoxybenzonitrile 124993-53-9 C8H7NO2
3-hydroxy-5-methoxybenzonitrile
—— tert-butyl 2'-oxospiro[azetidine-3,3'-indoline]-1-carboxylate 1251001-73-6 C15H18N2O3
tert-butyl 2'-oxospiro[azetidine-3,3'-indoline]-1-carboxylate
—— 4-cyano-4-(2,2,2-trifluoroacetylamino)piperidine-1-carboxylic acid tert-butyl ester 871115-20-7 C13H18F3N3O3
4-cyano-4-(2,2,2-trifluoroacetylamino)piperidine-1-carboxylic acid tert-butyl ester
—— 2,6-Dichloropyridine-4-sulfonyl chloride 1058741-91-5 C5H2Cl3NO2S
2,6-Dichloropyridine-4-sulfonyl chloride
—— 3-(Chloromethyl)pyrazole Hydrochloride 69658-97-5 C4H6Cl2N2
3-(Chloromethyl)pyrazole Hydrochloride
—— 6-bromo[1,2,4]triazolo[1,5-a]pyrimidine-2-carboxylic acid 300361-78-8 C6H3BrN4O2
6-bromo[1,2,4]triazolo[1,5-a]pyrimidine-2-carboxylic acid
—— 1-Phenyl-3-<2-phenylmercapto-aethyl>-thioharnstoff 13084-43-0 C15H16N2S2
1-Phenyl-3-<2-phenylmercapto-aethyl>-thioharnstoff
—— ethyl 2-(3,4-dihydro-2H-benzo[b][1,4]oxazin-3-yl)acetate 35990-53-5 C12H15NO3
ethyl 2-(3,4-dihydro-2H-benzo[b][1,4]oxazin-3-yl)acetate
—— (S)-2-amino-6-((4-methoxyphenyl)diphenylmethyl-amino)hexanoic acid 159857-61-1 C26H30N2O3
(S)-2-amino-6-((4-methoxyphenyl)diphenylmethyl-amino)hexanoic acid
—— (10S,13S)-17-Acetyl-10,13-dimethyl-6,7,8,10,12,13,14,15-octahydro-cyclopenta[a]phenanthren-3-one 117048-56-3 C21H24O2
(10S,13S)-17-Acetyl-10,13-dimethyl-6,7,8,10,12,13,14,15-octahydro-cyclopenta[a]phenanthren-3-one
—— 21-Acetoxy-1,4,9(11),16-pregnatetraen-3,20-dion 37413-91-5 C23H26O4
21-Acetoxy-1,4,9(11),16-pregnatetraen-3,20-dion
—— tert-butyl (4S)-5-amino-4-(benzyloxycarbonylamino)-5-oxopentanoate 17191-52-5 C17H24N2O5
tert-butyl (4S)-5-amino-4-(benzyloxycarbonylamino)-5-oxopentanoate
—— 2,6-dichloropyrimidin-4(3H)-one 120977-94-8 C4H2Cl2N2O
2,6-dichloropyrimidin-4(3H)-one
—— 3-azabicyclo[3.3.0]octane hydrochloride 112626-50-3 C7H13N*ClH
3-azabicyclo[3.3.0]octane hydrochloride
—— 1,8-dibromo-octane-2,7-dione 39095-41-5 C8H12Br2O2
1,8-dibromo-octane-2,7-dione
—— 5-bromoquinazolin-4(3H)-one 147006-47-1 C8H5BrN2O
5-bromoquinazolin-4(3H)-one
—— (R)-5-benzyl-2,2,3-trimethylimidazolidin-4-one 685128-77-2 C13H18N2O
(R)-5-benzyl-2,2,3-trimethylimidazolidin-4-one
—— 3-O-(4,4'-dimethoxytrityl)-1,2-dideoxy-D-ribose 401813-08-9 C26H28O5
3-O-(4,4'-dimethoxytrityl)-1,2-dideoxy-D-ribose
—— diphenylmethyl 7β-amino-7α-methoxy-3-<(1-methyl-1H-tetrazol-5-yl)thiomethyl>-3-cephem-4-carboxylate 56610-72-1 C24H24N6O4S2
diphenylmethyl 7β-amino-7α-methoxy-3-<(1-methyl-1H-tetrazol-5-yl)thiomethyl>-3-cephem-4-carboxylate
—— (+)-pinoresinol 4-O-glucopyranoside 24404-49-7 C26H32O11
(+)-pinoresinol 4-O-glucopyranoside