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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
—— 3-(4-chlorophenyl)-3-oxopropanoic acid 17589-68-3 C9H7ClO3
3-(4-chlorophenyl)-3-oxopropanoic acid
—— ethyl 3-oxo-2-<3-oxo-1,3-dihydroisobenzofuran-1-yl>butanoate 731773-32-3 C14H14O5
ethyl 3-oxo-2-<3-oxo-1,3-dihydroisobenzofuran-1-yl>butanoate
—— 1,4-bis((oxiran-2-ylmethoxy)methyl)benzene 29513-13-1 C14H18O4
1,4-bis((oxiran-2-ylmethoxy)methyl)benzene
—— 5-Dehydro-shikimisaeure 2922-42-1 C7H8O5
5-Dehydro-shikimisaeure
—— trans-1,2-Diamino-cyclohexan-N,N.N',N'-tetraessigsaeure 13291-61-7 C14H22N2O8
trans-1,2-Diamino-cyclohexan-N,N.N',N'-tetraessigsaeure
—— Methyl 3,4,6-Tri-O-acetyl-2-deoxy-2-phthalimido-1-thio-beta-D-glucopyranoside 79528-48-6 C21H23NO9S
Methyl 3,4,6-Tri-O-acetyl-2-deoxy-2-phthalimido-1-thio-beta-D-glucopyranoside
—— N-{6-(2-hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2H-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide 1931994-81-8 C20H21F3N4O4S
N-{6-(2-hydroxypropan-2-yl)-2-[2-(methylsulphonyl)ethyl]-2H-indazol-5-yl}-6-(trifluoromethyl)pyridine-2-carboxamide
—— 4'-bromo-2,6-dimethoxy-1,1'-biphenyl 168849-77-2 C14H13BrO2
4'-bromo-2,6-dimethoxy-1,1'-biphenyl
—— 9-(4-methylphenyl)fluorene 18153-43-0 C20H16
9-(4-methylphenyl)fluorene
—— (R)-(tetrahydrofuran-3-yl)hydrazine hydrochloride 1364632-31-4 C4H10N2O*ClH
(R)-(tetrahydrofuran-3-yl)hydrazine hydrochloride
—— 1-cyclobutylcyclopropanol 112650-60-9 C7H12O
1-cyclobutylcyclopropanol
—— methyl 3-bromopyrazolo[1,5-a]pyridine-5-carboxylate 1610611-84-1 C9H7BrN2O2
methyl 3-bromopyrazolo[1,5-a]pyridine-5-carboxylate
—— methyl 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazolo[1,5-a]pyridine-5-carboxylate 1610612-05-9 C15H19BN2O4
methyl 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazolo[1,5-a]pyridine-5-carboxylate
—— (E)-2-hydroxy-N’-((2-hydroxynaphthalen-1-yl)methylene)benzohydrazide 1099592-35-4 C18H14N2O3
(E)-2-hydroxy-N’-((2-hydroxynaphthalen-1-yl)methylene)benzohydrazide
—— bis(2-picolyl)phenylphosphine 86674-25-1 C18H17N2P
bis(2-picolyl)phenylphosphine
—— methyl 2,2-diallylpentan-2-carboxylate 824413-84-5 C12H18O2
methyl 2,2-diallylpentan-2-carboxylate
—— cis-Ru(Bpy)2Cl2·2H2O 15746-57-3 C10H8Cl2N2Ru*2H2O
cis-Ru(Bpy)2Cl2·2H2O
—— (E)-1-(3-methyl1-butenyl)boronic acid 70813-75-1 C5H11BO2
(E)-1-(3-methyl1-butenyl)boronic acid
—— 9-(4-(tert-butyl)phenyl)-9H-fluorene 651042-75-0 C23H22
9-(4-(tert-butyl)phenyl)-9H-fluorene
—— tert-butyl 2-[(diphenylmethylidene)amino]-5,6,7,8-tetrahydro-1,6-naphthyridine-6-carboxylate 1346673-94-6 C26H27N3O2
tert-butyl 2-[(diphenylmethylidene)amino]-5,6,7,8-tetrahydro-1,6-naphthyridine-6-carboxylate
—— (2R)-2',5'-difluoro-2-(3,4,5,6-tetrahydro-2H-pyran-2-yloxy)-propiophenone 241479-69-6 C14H16F2O3
(2R)-2',5'-difluoro-2-(3,4,5,6-tetrahydro-2H-pyran-2-yloxy)-propiophenone
—— ethyl butanethioate 20807-99-2 C6H12OS
ethyl butanethioate
—— (1S,12S)-7-Bromo-9-methoxy-14-oxo-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6,8,10(17),15-tetraene-4-carbaldehyde 122584-14-9 C17H16BrNO4
(1S,12S)-7-Bromo-9-methoxy-14-oxo-11-oxa-4-azatetracyclo[8.6.1.01,12.06,17]heptadeca-6,8,10(17),15-tetraene-4-carbaldehyde
—— 2,6-dichloro-1,4,5,8-naphthalenetetracarboxylic acid dianhydride 59723-21-6 C14H2Cl2O6
2,6-dichloro-1,4,5,8-naphthalenetetracarboxylic acid dianhydride
—— (E)-4-hydroxy-3-(3-(4-methoxyphenyl)acryloyl)-2H-chromen-2-one 1022282-99-0 C19H14O5
(E)-4-hydroxy-3-(3-(4-methoxyphenyl)acryloyl)-2H-chromen-2-one
—— 2-(4-chlorophenyl)-5-methylthiophene 95650-85-4 C11H9ClS
2-(4-chlorophenyl)-5-methylthiophene
—— 2-(2-Pyridyl)-4-benzyl-2-oxazoline 108915-08-8 C15H14N2O
2-(2-Pyridyl)-4-benzyl-2-oxazoline
—— 5,6-benzosalicylidene salicyloyl hydrazone 54009-54-0 C18H14N2O3
5,6-benzosalicylidene salicyloyl hydrazone
—— 2-(naphthalen-1-yloxymethyl)-2-dioctene acid 8-methyl ester 936221-69-1 C20H22O5
2-(naphthalen-1-yloxymethyl)-2-dioctene acid 8-methyl ester
—— 3-methoxy-1-naphthoic acid 147397-60-2 C12H10O3
3-methoxy-1-naphthoic acid
—— 1,2-bis(2,5-dimethylthien-3-yl)cyclopentene 219537-98-1 C17H20S2
1,2-bis(2,5-dimethylthien-3-yl)cyclopentene
—— potassium indole-3-acetate 2338-19-4 C10H8NO2*K
potassium indole-3-acetate
—— 6-(4-bromo-3-fluorophenyl)-1,2,4-triazin-3-amine 1029714-84-8 C9H6BrFN4
6-(4-bromo-3-fluorophenyl)-1,2,4-triazin-3-amine
—— 5-methyl-2-phenyl-4-[2-(1,3,3-trimethyl-1,3-dihydro-indol-2-ylidene)-ethylidene]-2,4-dihydro-pyrazol-3-one 5190-63-6 C23H23N3O
5-methyl-2-phenyl-4-[2-(1,3,3-trimethyl-1,3-dihydro-indol-2-ylidene)-ethylidene]-2,4-dihydro-pyrazol-3-one
—— ethyl 3-nitro-1H-pyrazole-5-carboxylate 39846-84-9 C6H7N3O4
ethyl 3-nitro-1H-pyrazole-5-carboxylate
—— 3-(pyrimidin-2-yl)thioazetidine 931581-82-7 C7H9N3S
3-(pyrimidin-2-yl)thioazetidine
—— ethyl (S)-2-amino-3,3-dimethylbutanoate 69557-34-2 C8H17NO2
ethyl (S)-2-amino-3,3-dimethylbutanoate
—— 5-isopropyloxazole-4-carboxylic acid 89006-96-2 C7H9NO3
5-isopropyloxazole-4-carboxylic acid
—— ethyl 6-hydroxy-5-methylpyrimidine-4-carboxylate 76480-52-9 C8H10N2O3
ethyl 6-hydroxy-5-methylpyrimidine-4-carboxylate
—— Prostaglandin A2 13345-50-1 C20H30O4
Prostaglandin A2
—— A<sub>2</sub> isoprostane 13345-50-1 C20H30O4
A<sub>2</sub> isoprostane
—— Prostaglandin A(2) 13345-50-1 C20H30O4
Prostaglandin A(2)
—— (+/-)-15-epi-prostaglandin A<sub>2</sub> 13345-50-1 C20H30O4
(+/-)-15-epi-prostaglandin A<sub>2</sub>
—— CIS-3-AMINOCYCLOBUTANECARBOXYLIC ACID 74316-27-1 C5H9NO2
CIS-3-AMINOCYCLOBUTANECARBOXYLIC ACID
—— cyclobutane-1,1-diylbis(methylene) bis(4-methylbenzenesulfonate) 22308-09-4 C20H24O6S2
cyclobutane-1,1-diylbis(methylene) bis(4-methylbenzenesulfonate)
—— (1S,3R,4R,7S)-3-(adenine-9-yl)-7-hydroxy-1-hydroxymethyl-2,5-dioxabicyclo[2.2.1]heptane 206055-70-1 C11H13N5O4
(1S,3R,4R,7S)-3-(adenine-9-yl)-7-hydroxy-1-hydroxymethyl-2,5-dioxabicyclo[2.2.1]heptane
—— methyl 1-benzyl-5-hydroxypiperidine-3-carboxylate 1269755-42-1 C14H19NO3
methyl 1-benzyl-5-hydroxypiperidine-3-carboxylate
—— (R)-piperazine-2-carboxylic acid dihydrochloride 126330-90-3 C5H10N2O2*2ClH
(R)-piperazine-2-carboxylic acid dihydrochloride
—— 5-methyl (S)-tert-butoxycarbonyl-3-dimethylaminomethylene-2-oxopyrrolidine-5-carboxylate 196394-47-5 C14H22N2O5
5-methyl (S)-tert-butoxycarbonyl-3-dimethylaminomethylene-2-oxopyrrolidine-5-carboxylate
—— (1S,3S)-3-hydroxycyclohexane-1-carboxylic acid 122743-44-6 C7H12O3
(1S,3S)-3-hydroxycyclohexane-1-carboxylic acid