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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
((5-噻唑基)甲基)-(4-硝基苯基)碳酸酯 4-nitrophenyl (thiazol-5-ylmethyl) carbonate 144163-97-3 C11H8N2O5S
((5-噻唑基)甲基)-(4-硝基苯基)碳酸酯
((4-羟基丁基)氮杂二基)双(己烷-6,1-二基)双(2-己基癸酸酯) ALC-0315 2036272-55-4 C48H95NO5
((4-羟基丁基)氮杂二基)双(己烷-6,1-二基)双(2-己基癸酸酯)
((3aR,4S,6aS)-5-乙酰氧基-2-氧代六氢-2H-环戊并[b]呋喃-4-基)甲基 乙酸酯 ((3aR,4S,5R,6aS)-5-acetoxy-2-oxohexahydro-2H-cyclopenta[b]furan-4-yl)methyl acetate 62939-82-6 C12H16O6
((3aR,4S,6aS)-5-乙酰氧基-2-氧代六氢-2H-环戊并[b]呋喃-4-基)甲基 乙酸酯
((3R,4S)-3-氟哌啶-4-基)氨基甲酸叔丁酯 tert-butyl N-[(3R,4S)-3-fluoropiperidin-4-yl]carbamate 1630815-57-4 C10H19FN2O2
((3R,4S)-3-氟哌啶-4-基)氨基甲酸叔丁酯
((3R,4R)-4-氨基四氢-2H-吡喃-3-基)氨基甲酸叔丁酯 tert-butyl ((3R,4R)-4-aminotetrahydro-2H-pyran-3-yl)carbamate 1240390-36-6 C10H20N2O3
((3R,4R)-4-氨基四氢-2H-吡喃-3-基)氨基甲酸叔丁酯
((3AR,4R,6R,6AR)-6-(4-(羟氨)-2-恶嘧啶-1(2H)-甲基)-2,2-二甲基四氢呋喃[3,4-D][1,3]二氧醇-4-基)异丁酸甲酯 molnupiravir acetonide 2346620-55-9 C16H23N3O7
((3AR,4R,6R,6AR)-6-(4-(羟氨)-2-恶嘧啶-1(2H)-甲基)-2,2-二甲基四氢呋喃[3,4-D][1,3]二氧醇-4-基)异丁酸甲酯
((2S)-2-氨基丙基)氨基甲酸叔丁酯 tert-butyl (S)-(2-aminopropyl)carbamate 121103-15-9 C8H18N2O2
((2S)-2-氨基丙基)氨基甲酸叔丁酯
((2R,3r,4r)-3-((4-氯苯甲酰基)氧基)-4-氟-4-甲基-5-氧代四氢呋喃-2-基)甲基4-氯苯甲酸 ((2R,3R,4R) 3-(4-chlorobenzoyloxy)-4-fluoro-4-methyl-5-oxotetrahydrofuran-2-yl)methyl-4-chlorobenzoate 1294481-79-0 C20H15Cl2FO6
((2R,3r,4r)-3-((4-氯苯甲酰基)氧基)-4-氟-4-甲基-5-氧代四氢呋喃-2-基)甲基4-氯苯甲酸
((2R,3R,4R)-3-(苯甲酰氧基)-4-氟-4-甲基-5-氧代四氢呋喃-2-基)苯甲酸甲酯 ((2R,3R,4R)-3-benzoyloxy-4-fluoro-4-methyl-5-oxo-tetrahydrofuran-2-yl)methyl benzoate 874638-80-9 C20H17FO6
((2R,3R,4R)-3-(苯甲酰氧基)-4-氟-4-甲基-5-氧代四氢呋喃-2-基)苯甲酸甲酯
((1R,3R,4R)-3-羟基-4-甲基环己基)氨基甲酸叔丁酯 tert-butyl ((1R,3R,4R)-3-hydroxy-4-methylcyclohexyl)carbamate 1403864-94-7 C12H23NO3
((1R,3R,4R)-3-羟基-4-甲基环己基)氨基甲酸叔丁酯
((1R,2S)-2-氨基环己基)氨基甲酸叔丁酯 tert-butyl ((1R,2S)-2-aminocyclohexyl)carbamate 364385-54-6 C11H22N2O2
((1R,2S)-2-氨基环己基)氨基甲酸叔丁酯
((1R,2R)-2-羟基-1-羟甲基-2-苯基乙基)氨基甲酸叔丁酯 ((1R,2R)-2-hydroxy-1-hydroxymethyl-2-phenylethyl)carbamic acid tert-butyl ester 1009093-14-4 C14H21NO4
((1R,2R)-2-羟基-1-羟甲基-2-苯基乙基)氨基甲酸叔丁酯
—— 2-Benzyloctahydro-1H-pyrrolo[3,4-c]pyridine hydrochloride 1187927-49-6 C14H21ClN2
2-Benzyloctahydro-1H-pyrrolo[3,4-c]pyridine hydrochloride
—— 6-cyanopyridin-2-ylboronic acid 848500-38-9 C6H5BN2O2
6-cyanopyridin-2-ylboronic acid
—— 3-O-β-Glucosyl-platycodigenin 38337-25-6 C36H58O12
3-O-β-Glucosyl-platycodigenin
—— (3-bromophenyl)dimethylphosphine oxide 60398-84-7 C8H10BrOP
(3-bromophenyl)dimethylphosphine oxide
—— 1-((trans)-4-methylcyclohexyl)ethanone 18446-90-7 C9H16O
1-((trans)-4-methylcyclohexyl)ethanone
—— (1S,5R)-5-Benzyloxymethyl-cyclopent-2-enol 668996-19-8 C13H16O2
(1S,5R)-5-Benzyloxymethyl-cyclopent-2-enol
—— trans-4-(Methylamino)cyclohexanol hydrochloride 923023-08-9 C7H15NO*ClH
trans-4-(Methylamino)cyclohexanol hydrochloride
—— 3,3-difluoro-2,2-dimethylpropanoic acid 1022154-50-2 C5H8F2O2
3,3-difluoro-2,2-dimethylpropanoic acid
—— tert-butyl-4-(methacryloyloxy)piperidine-1-carboxylate salt 1229727-38-1 C14H23NO4
tert-butyl-4-(methacryloyloxy)piperidine-1-carboxylate salt
—— 2-Ethynyl-6-(trifluoromethyl)pyrazine 1211529-10-0 C7H3F3N2
2-Ethynyl-6-(trifluoromethyl)pyrazine
—— 4-chloro-N-((R)-1-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)ethyl)benzamide 1923844-48-7 C24H24ClFN2O
4-chloro-N-((R)-1-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)ethyl)benzamide
—— N-(4-((6-azidohexyloxy)diphenylsilyloxy)butyl)-1-(5-((3aS,4S,6aR)-2-oxo-hexahydro-1H-thieno[3,4-d]imidazol-4-yl)-pentanamido)-3,6,9,12-tetraoxapentadecan-15-amide 1260247-50-4 C43H67N7O9SSi
N-(4-((6-azidohexyloxy)diphenylsilyloxy)butyl)-1-(5-((3aS,4S,6aR)-2-oxo-hexahydro-1H-thieno[3,4-d]imidazol-4-yl)-pentanamido)-3,6,9,12-tetraoxapentadecan-15-amide
—— 73428-45-2 C6H7N2O2
—— 1404074-90-3 C2F3O2*C7H13N2
—— 4-Pyridinol, 3,5-dibromo-, ion(1-) 141375-47-5 C5H2Br2NO
4-Pyridinol, 3,5-dibromo-, ion(1-)
—— 3-(3,5-dichloro-4-methoxybenzoyl)-1-oxo-2,3-dihydro-1,3-benzothiazole 1285573-47-8 C15H11Cl2NO3S
3-(3,5-dichloro-4-methoxybenzoyl)-1-oxo-2,3-dihydro-1,3-benzothiazole
—— 1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]indole-3-carbaldehyde 460355-03-7 C14H15NO4
1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]indole-3-carbaldehyde
—— 3-bromobenzofuran-2-carbonitrile 1357347-11-5 C9H4BrNO
3-bromobenzofuran-2-carbonitrile
—— 7'-fluoro-1',2'-dihydrospiro[cyclopropane -1,3-indole]-2'-one 872141-30-5 C10H8FNO
7'-fluoro-1',2'-dihydrospiro[cyclopropane -1,3-indole]-2'-one
—— 5-(bromomethyl)-2,3-dimethylpyrazine 1339947-51-1 C7H9BrN2
5-(bromomethyl)-2,3-dimethylpyrazine
—— 4-methoxy-1-piperidin-4-ylpiperidine hydrochloride 930604-26-5 C11H22N2O*ClH
4-methoxy-1-piperidin-4-ylpiperidine hydrochloride
—— bis(4-bromophenyl)phosphine oxide 15754-53-7 C12H9Br2OP
bis(4-bromophenyl)phosphine oxide
—— 5-(2-chloroacetamido)-2,4,6-triiodo-N,N'-bis(2,3-bis(2-chloroacetoxy)propyl)isophthalamide 155887-14-2 C24H23Cl5I3N3O11
5-(2-chloroacetamido)-2,4,6-triiodo-N,N'-bis(2,3-bis(2-chloroacetoxy)propyl)isophthalamide
—— Pubchem_57369830 70431-34-4 C11H21NNa3O7+3
Pubchem_57369830
—— sulfopin 2451481-08-4 C11H20ClNO3S
sulfopin
—— ethyl 4-bromo-5-methyl-1H-imidazole-2-carboxylate 1171125-20-4 C7H9BrN2O2
ethyl 4-bromo-5-methyl-1H-imidazole-2-carboxylate
—— 17-Alpha-cyano-9-alpha,17-beta-dihydroxyandrost-4-en-3-one 116256-35-0 C20H27NO3
17-Alpha-cyano-9-alpha,17-beta-dihydroxyandrost-4-en-3-one
—— 2-[(2R,3R)-2-Methanesulfinyl-4-oxo-3-(2-phenoxy-acetylamino)-azetidin-1-yl]-3-methyl-but-2-enoic acid 4-methoxy-benzyl ester 36760-29-9 C25H28N2O7S
2-[(2R,3R)-2-Methanesulfinyl-4-oxo-3-(2-phenoxy-acetylamino)-azetidin-1-yl]-3-methyl-but-2-enoic acid 4-methoxy-benzyl ester
—— Benzo[f]furo[3,2-c]quinoline 195-66-4 C15H9NO
Benzo[f]furo[3,2-c]quinoline
—— benzyl (S)-2-(((3-chloropyrazin-2-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate (benzyl (S)-2-(((3-chloropyrazin-2-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate) 2251014-87-4 C18H19ClN4O3
benzyl (S)-2-(((3-chloropyrazin-2-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate (benzyl (S)-2-(((3-chloropyrazin-2-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate)
—— D-Lysergic acid methyl ester 4579-64-0 C17H18N2O2
D-Lysergic acid methyl ester
—— 3,3,5-trifluoro-1H-pyrrolo[2,3-b]pyridin-2(3H)-one 1452561-47-5 C7H3F3N2O
3,3,5-trifluoro-1H-pyrrolo[2,3-b]pyridin-2(3H)-one
—— Quinoline sulfate 530-66-5 (bisulfate) C18H16N2O4S
Quinoline sulfate
—— 1,6-dimethyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid 934106-78-2 C9H9N3O2
1,6-dimethyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid
—— 7-bromo-5-fluoro-1H-pyrrolo[2,3-c]pyridine 1639977-12-0 C7H4BrFN2
7-bromo-5-fluoro-1H-pyrrolo[2,3-c]pyridine
—— Gpl23NZ2Q9 2061897-68-3 C34H38N4O5
Gpl23NZ2Q9
—— trans-Octahydro-1H-pyrrolo[3,4-b]pyridine 158060-81-2 C7H14N2
trans-Octahydro-1H-pyrrolo[3,4-b]pyridine
—— Ethyl-1-methyl-3-hydroxypyrrol-2-carboxylat 65171-90-6 C8H11NO3
Ethyl-1-methyl-3-hydroxypyrrol-2-carboxylat