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

DMAN CAS Registry Number: 20734-58-1 1,8-双二甲氨基萘

CAS Name: N,N,N',N'-Tetramethyl-1,8-naphthalenediamine
Additional Names: 1,8-bis(dimethylamino)naphthalene; proton sponge
Percent Composition: C 78.46%, H 8.47%, N 13.07%
Literature References: Prototype of a class of neutral aromatic diamines with exceptionally high basicity known as proton sponges. Prepn: W. G. Brown, N. J. Letang, J. Am. Chem. Soc. 63, 358 (1941); and basicity study: R. W. Alder et al., J. Chem. Soc. Chem. Commun. 1968, 723. X-ray crystal structure: H. Einspahr et al., Acta Crystallogr. B29, 1611 (1973). Proton transfer studies: F. Hibbert, J. Chem. Soc. Perkin Trans. 2 1974, 1862. Ab initio structural studies: J. A. Platts et al., J. Org. Chem. 59, 4647 (1994); and fluorescence spectroscopy: A. Szemik-Hojniak et al., J. Am. Chem. Soc. 120, 4840 (1998). Charge distribution: P. R. Mallinson et al., ibid. 121, 4640 (1999). 13C NMR study of hydrogen bonding: M. Pietrzak et al., ibid. 123, 4338 (2001). Catalytic activity: I. Rodriguez et al., J. Catal. 183, 14 (1999). Review of chemistry: H. A. Staab, T. Saupe, Angew. Chem. Int. Ed. 27, 865-879 (1988); R. W. Alder, Chem. Rev. 89, 1215-1223 (1989).

Eprosartan CAS Registry Number: 133040-01-4 依普罗沙坦

CAS Name: (aE)-a-[[2-Butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-yl]methylene]-2-thiophenepropanoic acid
Additional Names: (E)-3-[2-butyl-1-[(4-carboxyphenyl)methyl]-imidazol-5-yl]-2-(2-thi...
Literature References: Prototype of the imidazoleacrylic acid angiotensin II receptor antagonists. Prepn: J. A. Finkelstein et al., EP 403159 (1990 to SmithKline Beckman); eidem, US 5185351 (1993 to SmithKline Beecham); J. Weinstock et al., J. Med. Chem. 34, 1514 (1991); R. M. Keenan et al., ibid. 36, 1880 (1993). Pharmacology: R. M. Edwards et al., J. Pharmacol. Exp. Ther. 260, 175 (1992). Receptor binding study: H. T. Schambye et al., Mol. Pharmacol. 47, 425 (1995). Clinical pharmacokinetics: D. Tenero et al., Biopharm. Drug Dispos. 19, 351 (1998). Clinical trial in hypertension: W. J. Elliott et al., J. Hum. Hypertens. 13, 413 (1999). Review of clinical experience: L. Ruilope, B. Jäger, Expert Opin. Pharmacother. 4, 107-114 (2003).

Linezolid CAS Registry Number: 165800-03-3 利奈唑胺

CAS Name: N-[[(5S)-3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamideTrademarks: Zyvox (Pharmacia Upjohn); Zyvoxid (Pharmacia Upjohn)
Percent Composition: C 56.96%, H ...
Literature References: Prototype of the oxazolidinone antimicrobials; inhibits bacterial mRNA translation. Prepn: M. R. Barbachyn et al., WO 9507271 (1995 to Upjohn); eidem, US 5688792 (1997 to Pharmacia Upjohn); S. J. Brickner et al., J. Med. Chem. 39, 673 (1996). Antibacterial spectrum: C. W. Ford et al., Antimicrob. Agents Chemother. 40, 1508 (1996). Mechanism of action study: D. L. Shinabarger et al., ibid. 41, 2132 (1997). HPLC determn in plasma: C. Buerger et al., J. Chromatogr. B 796, 155 (2003). Clinical comparison with vancomycin, q.v., for MRSA infections: D. L. Stevens et al., Clin. Infect. Dis. 34, 1481 (2002). Review of pharmacology: L. D. Dresser, M. J. Rybak, Pharmacotherapy 18, 456-462 (1998); and clinical experience: R. Norrby, Expert Opin. Pharmacother. 2, 293-302 (2001).

Rolipram CAS Registry Number: 61413-54-5 咯利普兰

CAS Name: 4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinonePercent Composition: C 69.79%, H 7.69%, N 5.09%, O 17.43%
Literature References: Prototypical selective phosphodiesterase 4 (PDE4) inhibitor. Prepn: BE 826923; R. Schmiechen et al., US 4193926 (1975, 1980 both to Schering AG). Selective enzyme inhibition and enhancement of cAMP accumulation in rat brain tissue: U. Schwabe et al., Mol. Pharmacol. 12, 900 (1976). Antidepressant mechanism of action study: H. Wachtel, Neuropharmacology 22, 267 (1983). Receptor binding study: H. H. Schneider et al., Eur. J. Pharmacol. 127, 105 (1986). Pharmacokinetics: W. Krause, G. Kühne, Xenobiotica 18, 561 (1988). Clinical evaluation in severe depression: F. Eckmann et al., Curr. Ther. Res. 43, 291 (1988). Pharmacology and efficacy in exptl autoimmune encephalomyelitis: N. Sommer et al., Nat. Med. 1, 244 (1995).

Helenalin CAS Registry Number: 6754-13-8 心菊内酯

CAS Name: [3aS-(3aa,4a,4ab,7aa,8a,9aa)]-3,3a,4,4a,7a,8,9,9a-Octahydro-4-hydroxy-4a,8-dimethyl-3-methyleneazuleno[6,5-b]furan-2,5-dione
Additional Names: 6a,8b-dihydroxy-4-oxoambrosa-2,11(13)-di...
Literature References: Pseudoguaianolide sesquiterpenoid lactone from Helenium autumnale L., H. amarum (Raf.) H. Roch, H. microcephalum DC., Compositae. Isoln: Clark, J. Am. Chem. Soc. 58, 1982 (1936); and characterization: Adams, Herz, ibid. 71, 2546 (1949). Structure: Büchi, Rosenthal, ibid. 78, 3860 (1956); Barton, de Mayo, Q. Rev. Chem. Soc. 11, 189 (1957); Herz, J. Org. Chem. 27, 4043 (1962). Abs config studies: Herz, Kagan, ibid. 32, 216 (1967). Synthesis of racemic form: Y. Ohfune et al., J. Am. Chem. Soc. 100, 5946 (1978); M. R. Roberts, R. H. Schlessinger, ibid. 101, 7626 (1979); C. H. Heathcock et al., ibid. 104, 1907 (1982). Toxicity study: D. A. Witzel et al., Am. J. Vet. Res. 37, 859 (1976).

Acarbose CAS Registry Number: 56180-94-0 阿卡波糖

CAS Name: O-4,6-Dideoxy-4-[[[1S-(1a,4a,5b,6a)]-4,5,6-trihydroxy-3-(hydroxymethyl)-2-cyclohexen-1-yl]amino]-a-D-glucopyranosyl-(1®4)-O-a-D-glucopyranosyl-(1®4)-D-glucose
Additional Names: 4'',6'...
Literature References: Pseudotetrasaccharide containing an unsaturated cyclitol moiety. An a-glucosidase inhibitor that reduces sugar absorption in the gastrointestinal tract. Isoln from strains of Actinoplanes: W. Frommer et al., DE 2347782; eidem, US 4062950 (1975, 1977 both to Bayer). Total synthesis: S. Ogawa, Y. Shibata, Chem. Commun. 1988, 605; eidem, Carbohydr. Res. 189, 309 (1989). Biosynthetic studies: U. Degwert et al., J. Antibiot. 40, 855 (1987). Glucosidase inhibition studies: D. D. Schmidt et al., Naturwissenschaften 64, 535 (1977); W. Puls et al., ibid. 536. Use in treatment of diabetic adults: D. Sailor, G. Roder, Arzneim.-Forsch. 30, 2182 (1980); H. Laube et al., ibid. 1154. Long-term study in sulfonylurea-treated diabetics: H. Vierhapper et al., Diabetologia 20, 586 (1981). Potential use in prophylaxis of dental caries: N. E. Fiehn, D. Moe, Scand. J. Dent. Res. 90, 124 (1982). Review of pharmacodynamics, pharmacokinetics and therapeutic potential: S. P. Clissold, C. Edwards, Drugs 35, 214-243 (1988).

Mepiprazole CAS Registry Number: 20326-12-9 美吡哌唑

CAS Name: 1-(3-Chlorophenyl)-4-[2-(5-methyl-1H-pyrazol-3-yl)ethyl]piperazine
Additional Names: 3-[2-(N'-m-chlorophenylpiperazino)ethyl]-5-methylpyrazolePercent Composition: C 63.04%, H 6.94%, C...
Literature References: Psychotropic agent with CNS-depressant effects. Prepn: V. Koppe et al., GB 1124710; eidem, US 3491097 (1968, 1970 both to E. Merck); eidem, Eur. J. Med. Chem. 10, 154, 162 (1975). Pharmacological study: M. A. Ruch-Monachon et al., Arch. Int. Pharmacodyn. Ther. 219, 326 (1976). Effects on brain biogenic amine metabolism: C. Seyfried et al., Arzneim.-Forsch. 26, 1088 (1976). EEG effects in rabbits: S. Watanabe et al., ibid. 29, 274 (1979).

Metapramine CAS Registry Number: 21730-16-5 美他帕明

CAS Name: 10,11-Dihydro-N,5-dimethyl-5H-dibenz[b,f]azepin-10-amine
Additional Names: 10,11-dihydro-5-methyl-10-(methylamino)-5H-dibenz[b,f]azepineTrademarks: Timaxel (Rhe-Poulenc)
Percent Co...
Literature References: Psychotropic agent, related structurally to imipramine, q.v. Prepn: J. C. Fouche, C. G. A. Gueremy, ZA 6800345 corresp to US 3622565 (1968, 1971 both to Rhone-Poulenc). Determn in plasma by GC: A. R. Viala et al., Anal. Chem. 49, 2354 (1977). HPLC method: J. P. Sommadossi et al., J. Chromatogr. 228, 205 (1982). Pharmacological and clinical effects: P. Dick, Encephale 4, 41 (1978). Clinical studies: L. F. Gayral et al., ibid. 365; E. J. Caille, J.-P. Brun, Psychol. Med. 13, 1879 (1981). Biotransformation in animals and man: B. Decouvelaere et al., Therapie 37, 249 (1982).

Etoperidone CAS Registry Number: 52942-31-1 依托哌酮

CAS Name: 2-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-4,5-diethyl-2,4-dihydro-3H-1,2,4-triazol-3-one
Percent Composition: C 60.39%, H 7.47%, Cl 9.38%, N 18.53%, O 4.23%
Literature References: Psychotropic drug related structurally to trazodone, q.v. Prepn: G. Palazzo, DE 2351739; idem, US 3857845 (both 1974 to Angelini). Pharmacology and acute toxicity: R. Lisciani et al., Arzneim.-Forsch. 28, 417 (1978); M. T. Ramacci et al., ibid. 29, 294 (1979). Clinical evaluation: P. Bertoletti, G. Clin. Med. 58, 393 (1977). Teratology study: S. Barcellona et al., Toxicology 8, 87 (1977). Acute cardiovascular toxicity study: R. Lisciani et al., ibid. 10, 151 (1978).

Lofepramine CAS Registry Number: 23047-25-8 洛非帕明

CAS Name: 1-(4-Chlorophenyl)-2-[[3-(10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]methylamino]ethanone
Additional Names: 4'-chloro-2-[[3-(10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]methyla...
Literature References: Psychotropic drug related to imipramine, q.v. Prepn: E. Eriksoo et al., GB 1177525; eidem, US 3637660 (1970, 1972 both to AB Leo). Chemistry and pharmacology: E. Eriksoo, O. Rohte, Arzneim.-Forsch. 20, 1561 (1970). Absorption and metabolism: J. R. Tulic et al., Acta Pharmacol. Toxicol. 32, 304 (1973). Distribution and excretion: G. Plym Forshell, Xenobiotica 5, 73 (1975). Pharmacokinetics: G. Plym Forshell et al., Eur. J. Clin. Pharmacol. 9, 291 (1976). Clinical study: S. Wright, L. Herrmann, Arzneim.-Forsch. 26, 1167 (1976).