其它产品项目整合

项目整合的本质是一项集合成方法学、反应工程学与过程分析技术于一体的系统工程。其核心逻辑可以概括为以下几点：源头优选：利用如N-硝胺化学等底层方法学突破，从分子层面颠覆传统高成本、高污染路线。过程强化：依托连续流技术，攻克有机金属试剂应用、光化学反应放大等“不可能”任务，实现高危工艺的本质安全。系统集成：整合“反应-淬灭-分离”全流程，利用微流控与在线分析技术，消除批次间的差异，实现药品制造的连续化与智能化。当前，中间体工艺研发正在经历从“经验驱动”向“数据驱动”的转变。AI辅助路线设计、自动化高通量筛选与连续制造平台的结合，将使得“分子结构与最优工艺路径”之间的映射关系逐渐清晰。未来的竞争优势，将属于那些能够将底层化学创新与先进工程技术进行无缝整合的研发体系。
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其它产品项目整合

Panipenem CAS Registry Number: 87726-17-8 帕尼培南

CAS Name: (5R,6S)-6-[(1R)-1-Hydroxyethyl]-3-[[(3S)-1-(1-iminoethyl)-3-pyrrolidinyl]thio]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
Additional Names: (5R,6S)-6-[(R)-1-hydroxyethyl]-2...
Literature References: Carbapenem antibiotic. Prepn: T. Miyadera et al., J. Antibiot. 36, 1034 (1983). Manufacturing process: A. Yoshida, K. Oda, EP 587436 (1994 to Sankyo). Antibacterial spectrum in vitro: H. C. Neu et al., Antimicrob. Agents Chemother. 30, 828 (1986). Series of articles on pharmacology and clinical efficacy in combination with betamipron, q.v: Chemotherapy (Tokyo) 39 Suppl 3, 1-813 (1991). Toxicology: K. Kimura et al., ibid. 140.

Acetazolamide CAS Registry Number: 59-66-5 乙酰唑胺

CAS Name: N-[5-(Aminosulfonyl)-1,3,4-thiadiazol-2-yl]acetamide
Additional Names: 5-acetamido-1,3,4-thiadiazole-2-sulfonamide; 2-acetylamino-1,3,4-thiadiazole-5-sulfonamideTrademarks: Acetamox (...
Literature References: Carbonic anhydrase inhibitor. Prepn: R. O. Roblin, J. W. Clapp, J. Am. Chem. Soc. 72, 4890 (1950); J. W. Clapp, R. O. Roblin, US 2554816 (1951 to Am. Cyanamid). HPLC determn in pharmaceuticals: Z. S. Gomaa, Biomed. Chromatogr. 7, 134 (1993). Effect on retinal circulation: S. M. B. Rassam et al., Eye 7, 697 (1993). Clinical trial in postoperative elevation of intraocular pressure: I. D. Ladas et al., Br. J. Ophthalmol. 77, 136 (1993). Comprehensive description: J. Parasrampuria, Anal. Profiles Drug Subs. Excip. 22, 1-32 (1993). Review of efficacy in acute mountain sickness: L. D. Ried et al., J. Wilderness Med. 5, 34-48 (1994).

Brinzolamide CAS Registry Number: 138890-62-7 布林佐胺

CAS Name: (4R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxideTrademarks: Azopt (Alcon)
Percent Composition: C 37.58%, H 5.52%, N 10.96%, ...
Literature References: Carbonic anhydrase inhibitor. Prepn: T. R. Dean et al., WO 9115486; eidem, US 5378703 (1991, 1995 both to Alcon). Clinical trial: L. H. Silver, Am. J. Ophthalmol. 126, 400 (1998).

Butazolamide CAS Registry Number: 16790-49-1 布他唑胺

CAS Name: N-[5-(Aminosulfonyl)-1,3,4-thiadiazol-2-yl]butanamide
Additional Names: N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)butyramide; 5-butyramido-1,3,4-thiadiazole-2-sulfonamideTrademarks: Butami...
Literature References: Carbonic anhydrase inhibitor. Prepn: Vaughan et al., J. Org. Chem. 21, 700 (1956); GB 769757 (1957 to Am. Cyanamid).

Methazolamide CAS Registry Number: 554-57-4 醋甲唑胺

CAS Name: N-[5-(Aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene]acetamide
Additional Names: N-(4-methyl-2-sulfamoyl-D2-1,3,4-thiadiazolin-5-ylidene)acetamide; 5-acetylamino-4-methyl-D2-1...
Literature References: Carbonic anhydrase inhibitor. Prepn: Young et al., J. Am. Chem. Soc. 78, 4649 (1956); US 2783241 (1957 to Am. Cyanamid); Pala, Farmaco Ed. Sci. 13, 650 (1958).

Peruvoside CAS Registry Number: 1182-87-2 黄夹次苷

CAS Name: (3b,5b)-3-[(6-Deoxy-3-O-methyl-a-L-glucopyranosyl)oxy]-14-hydroxy-19-oxocard-20(22)-enolide
Additional Names: cannogenin a-L-thevetoside
Trademarks: Encordin (Merck KGaA)
Percen...
Literature References: Cardenolide (cardiac glycoside) found in seeds of the tropical garden plant Thevetia peruviana (Pers.) K. Schum. (Th. neriifolia Juss.), Apocynaceae (named trumpet flower in Florida). Isoln: Rangaswami, Venkata Rao, J. Sci. Ind. Res. 17B, 331 (1958). Structure: Bloch et al., Helv. Chim. Acta 43, 652 (1960). Pharmacological studies: Arzneim.-Forsch. 18, 1582-1608 (1968).

Diginatin CAS Registry Number: 52589-12-5 毛地黄杂质E

CAS Name: (3b,5b,12b,16b)-3-[(O-2,6-Dideoxy-b-D-ribo-hexopyranosyl-(1®4)-O-2,6-dideoxy-b-D-ribo-hexopyranosyl-(1®4)-2,6-dideoxy-b-D-ribo-hexopyranosyl)oxy]-12,14,16-trihydroxy-card-20(22)-enolide<...
Literature References: Cardiac glycoside from Digitalis lanata Ehrk., Scrophulariaceae: Murphy, J. Am. Pharm. Assoc. Sci. Ed. 44, 719 (1955); Angliker et al., Ann. 607, 131 (1957); von Wartburg et al., Experientia 14, 439 (1958). Acid hydrolysis yields 1 mol diginatigenin + 3 mols D-digitoxose. The sugar residue is attached to the hydroxyl group at C-3 of the aglycon.

Hellebrin CAS Registry Number: 13289-18-4 嚏根草因

CAS Name: 3-[(6-Deoxy-4-O-b-D-glucopyranosyl-a-L-mannopyranosyl)oxy]-5,14-dihydroxy-19-oxobufa-20,22-dienolide
Additional Names: hellebrigenin glucorhamnoside
Percent Composition: C 59.66%, ...
Literature References: Cardiac glycoside isolated from rhizome of Helleborus niger L., Ranunculaceae: Karrer, Festschr. Emil Barell 1936, 238, C.A. 31, 23488 (1937). Structure: Karrer, Helv. Chim. Acta 26, 1353 (1943); Wissner, Kating, Planta Med. 20, 344 (1971).

Neriifolin CAS Registry Number: 466-07-9 黄夹次甙乙

CAS Name: (3b,5b)-3-[(6-Deoxy-3-O-methyl-a-L-glucopyranosyl)oxy]-14-hydroxycard-20(22)-enolide
Percent Composition: C 67.39%, H 8.67%, O 23.94%
Literature References: Cardiac glycoside isolated from Thevetia neriifolia Juss.: M. Frèrejacque, Compt. Rend. 221, 645 (1945); from Cerbera odollam Gaertn.: S. Rangaswami, E. V. Rao, J. Sci. Ind. Res. 16B, 209 (1957); from Thevetia thevetioides seeds: J. L. McLaughlin et al., J. Econ. Entomol. 73, 39 (1980). Pharmacology: K. Mezey, Arch. Int. Pharmacodyn. Ther. 84, 367 (1950); K. K. Chen et al., ibid. 81.

Deslanoside CAS Registry Number: 17598-65-1 去乙酰毛花苷

CAS Name: (3b,5b,12b)-3-[(O-b-D-Glucopyranosyl-(1®4)-O-2,6-dideoxy-b-D-ribo-hexopyranosyl-(1®4)-O-2,6-dideoxy-b-D-ribo-hexopyranosyl-(1®4)-2,6-dideoxy-b-D-ribo-hexopyranosyl)oxy]-12,14-dihydroxyca...
Literature References: Cardiac glycoside. Isoln from leaves of Digitalis lanata Ehrh., Scrophulariaceae: Stoll, Kreis, Helv. Chim. Acta 16, 1049, 1390 (1933). Prepn by alkaline degradation of lanatoside C: Kroszczynski et al., Acta Pol. Pharm. 21, 357 (1964), C.A. 62, 10292b (1965). Hemodynamic effects in heart failure: E. Ambrosioni et al., Int. J. Clin. Pharmacol. Biopharm. 17, 416 (1979). Clinical pharmacokinetics: A. Marzo et al., Farmaco Ed. Prat. 37, 28 (1982). Determn in blood and urine by HPLC/MS/MS: F. Guan et al., Anal. Chem. 71, 4034 (1999).