原料药中间体是指在药物合成过程中用于生成最终活性成分(即原料药)的化学物质。这些中间体在制药工业中扮演着重要角色,它们通过一系列化学反应逐步转化成成品药物。根据其在生产过程中的位置和功能,可以将原料药中间体分为以下几个类别:
起始物料:这类中间体是最初用于合成最终产品的原材料。它们通常来源于天然产物、化工产品或其他已经存在的化合物。
关键中间体:这些中间体在整个合成过程中起着核心作用,通常是通过复杂的化学反应得到的。它们对于确保原料药的质量和成本效益至关重要。
保护基团:在药物合成中使用这类中间体是为了对某些敏感部分进行临时性或选择性的“保护”,防止它们在不必要的位置上发生副反应。保护完成后可通过特定条件去除这些保护基。
催化剂和添加剂:虽然不直接形成最终产品,但这些物质能够促进化学反应、提高产率或改善产品的质量特性。
分离纯化溶剂:这类中间体主要用于原料药合成过程中的提纯步骤。它们帮助从目标产物中去除杂质并提高产品的纯度。
选择合适的原料药中间体对于保证药物的安全性和有效性至关重要,因此,在其开发过程中需要考虑多个因素,包括成本效益、反应条件的可控性以及环境友好型等方面。
| 中文名称 | 英文名称 | CAS号 | 化学式 |
|---|---|---|---|
| 7-氨基-3-{[(5-甲基-1,3,4-噻二唑-2-基)硫]甲基}头孢霉素烷酸 | (6R,7R)-7-amino-3-(5-methyl-1,3,4-thiadiazol-2-ylthiomethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid | 30246-33-4 | C11H12N4O3S3 |
| 7-氨基-3-(1-甲基-1H-四唑-5-硫代甲基)-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸 | (6R,7R)-7-amino-3-[(1H-1-methyltetrazol-5-yl)thio]methylceph-3-em-4-carboxylic acid | 24209-38-9 | C10H12N6O3S2 |
| 7-氨基-2(3H)-苯并恶唑酮 | 7-aminobenzo[d]oxazol-2(3H)-one | 81282-60-2 | C7H6N2O2 |
| 7-氧代-2,6-二氮杂螺[3,4]辛烷-2-甲酸叔丁酯 | tert-butyl 7-oxo-2,6-diazaspiro[3.4]octane-2-carboxylate | 1234616-51-3 | C11H18N2O3 |
| 7-氟萘-1-醇 | 7-fluoronaphthalen-1-ol | 3132-92-1 | C10H7FO |
| 7-氟喹啉-6-甲腈 | 7-fluoroquinoline-6-carbonitrile | 956901-17-0 | C10H5FN2 |
| 7-氟吲哚 | 7-fluoro-1H-indole | 387-44-0 | C8H6FN |
| 7-氟-6-硝基-4-羟基喹唑啉 | 7-fluoro-6-nitro-3H-quinazolin-4-one | 162012-69-3 | C8H4FN3O3 |
| 7-氟-1-茚满酮 | 7-fluoro-2,3-dihydro-1H-inden-1-one | 651735-59-0 | C9H7FO |
| 7-氟-1-四氢萘酮 | 7-fluoro-3,4-dihydronaphthalen-1(2H)-one | 2840-44-0 | C10H9FO |
| 7-氟-1,4-二氢-1-[(1S)-1-(羟基甲基)-2-甲基丙基]-6-碘-4-氧代-3-喹啉甲酸乙酯 | 7-fluoro-1-((S)-1-hydroxymethyl-2-methylpropyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid ethyl ester | 697762-60-0 | C17H19FINO4 |
| 7-噁-3,9-二氮杂双环[3.3.1]壬烷-3-羧酸叔丁酯 | tert-butyl 3-oxa-7,9-diazabicyclo[3.3.1]nonane-7-carboxylate | 864448-41-9 | C11H20N2O3 |
| 7-叔丁氧基-7-氧代庚酸 | 7-(tert-butoxy)-7-oxoheptanoic acid | 1469894-57-2 | C11H20O4 |
| 7-乙基-10-羟基喜树碱中间体 | (4S)-4-ethyl-7,8-dihydro-4-hydroxy-1H-pyrano[3,4-f]indolizine-3,6,10(4H)-trione | 110351-94-5 | C13H13NO5 |
| 7-三氟甲基-1-四氢萘酮 | 7-trifluoromethyl-1-tetralone | 54752-50-0 | C11H9F3O |
| 7-[(3-氯-6,11-二氢-6-甲基-5,5-二氧代二苯并[c,f][1,2]硫氮杂卓-11-基)氨基]庚酸硫酸盐水合物(2:1:2) | Tianeptine hemisulfate monohydrate | 1224690-84-9 | C42H56Cl2N4O14S3 |
| 7-Boc-3-溴-5,6,7,8-四氢-1,2,4-三唑并[4,3-a]吡嗪 | tert-butyl 3-bromo-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine-7(8H)-carboxylate | 723286-80-4 | C10H15BrN4O2 |
| 7-(二乙基氨基)-4-(羟基甲基)-2H-苯并吡喃-2-酮 | 7-(diethylamino)-4-(hydroxymethyl)-2H-chromen-2-one | 54711-38-5 | C14H17NO3 |
| 7-(3-氯丙氧基)-4-[(2,4-二氯-5-甲氧基苯基)氨基]-6-甲氧基-3-氰基喹啉 | 7-(3-chloropropoxy)-4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxyquinoline-3-carbonitrile | 380844-49-5 | C21H18Cl3N3O3 |
| 7-(2,2-二苯基乙烯基)-1,2,3,3A,4,8B-六氢-4-(4-甲基苯基)-环戊丙[B]吲哚 | 7-(2,2-Diphenylvinyl)-4-(p-tolyl)-1,2,3,3a,4,8b-hexahydrocyclopenta[b]indole | 213670-22-5 | C32H29N |
| 7,8-二羟基-4-苯基香豆素 | 7,8-dihydroxy-4-phenyl-2H-chromen-2-one | 842-01-3 | C15H10O4 |
| 7,8-二甲氧基-3-(3-氯丙基)-1,3-二氢-2H-3-苯并氮杂卓-2-酮 | 7,8-dimethoxy-3-(3-chloropropyl)-1,3-dihydro-2H-3-benzazepin-2-one | 85175-59-3 | C15H18ClNO3 |
| 7,8-二氟-6,11-二氢二苯并[b,e]噻吩-11-醇 | 7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-ol | 1985607-83-7 | C14H10F2OS |
| 7,11-二乙基-10-羟基喜树碱 | 7,11-Diethyl-10-hydroxycamptothecin | 947687-01-6 | C24H24N2O5 |
| 6beta-羟基莫米松糠酸盐 | 6beta-Hydroxy Mometasone Furoate | 132160-74-8 | C27H30Cl2O7 |
| 6-酮雌二醇 | 6-ketoestradiol | 571-92-6 | C18H22O3 |
| 6-脒-2-萘酚 甲基磺酸 | 6-amidino-2-naphthol methanesulfonate | 82957-06-0 | CH4O3S*C11H10N2O |
| 6-羧基吲哚酮 | 2-oxoindoline-6-carboxylic acid | 334952-09-9 | C9H7NO3 |
| 6-羟基黄体酮 | 6ζ-hydroxypregn-4-ene-3,20-dione | 604-20-6 | C21H30O3 |
| 6-羟基色满酮 | 6-hydroxychroman-4-one | 80096-64-6 | C9H8O3 |
| 6-羟基-N-甲基-1-萘羧酰胺 | 6-hydroxy-N-methyl-1-naphthalenecarboxamide | 847802-91-9 | C12H11NO2 |
| 6-碘苯并二氢吡喃e | 6-iodochromane | 67856-45-5 | C9H9IO |
| 6-碘-4(H)-喹唑啉酮 | 6-iodoquinazolin-4(3H)-one | 16064-08-7 | C8H5IN2O |
| 6-碘-1H-吲唑 | 6-Iodo-1H-indazole | 261953-36-0 | C7H5IN2 |
| 6-硝基香豆素 | 6-nitrocoumarin | 2725-81-7 | C9H5NO4 |
| 6-硝基-1-茚满酮 | 6-nitroindan-1-one | 24623-24-3 | C9H7NO3 |
| 6-硝基-1,4-苯并二氧杂环 | 6-nitro-2,3-dihydrobenzo[b][1,4]dioxine | 16498-20-7 | C8H7NO4 |
| 6-甲氧基靛红 | 6-methoxyisatin | 52351-75-4 | C9H7NO3 |
| 6-甲氧基苯并噻唑 | 6-methoxy-1,3-benzothiazole | 2942-13-4 | C8H7NOS |
| 6-甲氧基-7-((1-甲基哌啶-4-基)甲氧基)喹唑啉-4(3h)-酮 | 6-methoxy-7-(N-methyl-4-piperidinylmethoxy)-3,4-dihydroquinazolin-4-one | 264208-69-7 | C16H21N3O3 |
| 6-甲氧基-4-羧酸喹啉 | 6-methoxyquinoline-4-carboxylic acid | 86-68-0 | C11H9NO3 |
| 6-甲氧基-2-肟-1-茚酮 | (2E)-2-(hydroxyimino)-6-methoxy-2,3-dihydro-1H-inden-1-one | 24077-98-3 | C10H9NO3 |
| 6-甲基-4-氧-5,6-二氢-4H-噻吩并[2,3-b]噻喃-2-磺酰胺 | 5,6-dihydro-4H-6-methylthieno[2,3-b]thiopyran-4-one-2-sulfonamide | 120279-88-1 | C8H9NO3S3 |
| 6-甲基-2-吡啶基-2-乙酰氨基-2-脱氧-b-D-巯基吡喃糖苷 | N-((2S,3R,4R,5S,6R)-4,5-Dihydroxy-6-(hydroxymethyl)-2-((6-methylpyridin-2-yl)thio)tetrahydro-2H-pyran-3-yl)acetamide | 149263-94-5 | C14H20N2O5S |
| 6-溴香兰素 | 6-bromovanillin | 60632-40-8 | C8H7BrO3 |
| 6-溴茚酮 | 6-bromoindan-1-one | 14548-39-1 | C9H7BrO |
| 6-溴苯并[D]噁唑 | 6-bromobenzo[d]oxazole | 375369-14-5 | C7H4BrNO |
| 6-溴喹啉-4-羧酸 | 6-bromoquinoline-4-carboxylic acid | 160233-76-1 | C10H6BrNO2 |
| 6-溴-7-羟基-4-(羟甲基)香豆素 | 6-bromo-7-hydroxy-4-hydroxymethylcoumarin | 223420-41-5 | C10H7BrO4 |
| 6-溴-5-(2-氟-4-硝基苯氧基)-1-甲基-1H-吲唑 | 6-bromo-5-(2-fluoro-4-nitrophenoxy)-1-methyl-1H-indazole | 1206800-24-9 | C14H9BrFN3O3 |