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

Guaiapate CAS Registry Number: 852-42-6 愈创哌特

CAS Name: 1-[2-[2-[2-(2-Methoxyphenoxy)ethoxy]ethoxy]ethyl]piperidineTrademarks: Klamar (Maggioni)
Percent Composition: C 66.84%, H 9.04%, N 4.33%, O 19.79%
Literature References: Basic ether deriv of guaiacol, q.v. Prepn: M. Carissimi, F. Ravenna, FR 1386633; eidem, US 3320254 (1965, 1967 both to Maggioni); M. Carissimi et al., J. Med. Chem. 8, 542 (1965). Pharmacological and clinical studies: G. Barbi, Gazz. Med. Ital. 127, 13 (1968). Analytical study: S. Cavicchi et al., Boll. Chim. Farm. 108, 682 (1969).

DMAP CAS Registry Number: 1122-58-3 4-二甲氨基吡啶

CAS Name: N,N-Dimethyl-4-pyridinamine
Additional Names: 4-(dimethylamino)pyridine
Percent Composition: C 68.82%, H 8.25%, N 22.93%
Literature References: Basic nucleophilic catalyst. Prepn: E. Koenigs et al., Ber. 58, 2571 (1925). Fluorescence spectra: S. Mishina et al., J. Photochem. Photobiol. A 141, 153 (2001). Use in Baylis-Hillman chemistry: K. Y. Lee et al., Bull. Korean Chem. Soc. 23, 659 (2002); in olefin hydroxylations: Q. Yao, Org. Lett. 4, 2197 (2002); in regioselective acylations: T. Kurahashi et al., Tetrahedron 58, 8669 (2002). Review of early literature and use in acylation chemistry: G. Höfle et al., Angew. Chem. Int. Ed. 17, 569-583 (1978); U. Ragnarsson, L. Grehn, Acc. Chem. Res. 31, 494-501 (1998); and of alkylation: E. F. V. Scriven, Chem. Soc. Rev. 12, 129-161 (1983). Brief description and synthetic uses: A. Hassner, "4-(Dimethylamino)pyridine" in Encyclopedia of Reagents for Organic Synthesis 3, L. A. Paquette, Ed. (John Wiley Sons, New York, 1995) pp 2022-2023.

Netropsin CAS Registry Number: 1438-30-8 纺锤菌素

CAS Name: 4-[[[(Aminoiminomethyl)amino]acetyl]amino]-N-[5-[[(3-amino-3-iminopropyl)amino]carbonyl]-1-methyl-1H-pyrrol-3-yl]-1-methyl-1H-pyrrole-2-carboxamide
Additional Names: N'-(2-amidinoethy...
Literature References: Basic oligopeptide antibiotic produced by Streptomyces netropsis with wide range of antimicrobial activity. Prepn and antibacterial spectrum: A. C. Finlay et al., J. Am. Chem. Soc. 73, 341 (1951); and trypanocidal activity: C. Cosar et al., Compt. Rend. 234, 1498 (1952). Antiviral activity: F. M. Schabel et al., Proc. Soc. Exp. Biol. Med. 83, 1 (1953). Identity with sinanomycin: K. Watanabe, J. Antibiot. 9A, 102 (1956). Structural studies: M. Julia, N. Joseph, Compt. Rend. 243, 961 (1956). Structure: C. W. Waller et al., J. Am. Chem. Soc. 79, 1265 (1957). Revised structure: M. Julia, N. Préau-Joseph, Compt. Rend. 257, 1115 (1963); eidem, Bull. Soc. Chim. Fr. 1967, 4348. Specific binding to DNA: Ch. Zimmer et al., J. Mol. Biol. 58, 329 (1971); K. Zakrzewska et al., Nucleic Acids Res. 11, 8825, 8841 (1983). Use in gradient separation of DNA: K. M. Tatti et al., Anal. Biochem. 89, 561 (1978). Selective blocking of DNAase I cleavage: Ch. Zimmer et al., Nucleic Acids Res. 8, 2999 (1980). Review of activity: F. E. Hahn in Antibiotics vol. 3, J. W. Corcoran, F. E. Hahn, Eds. (Springer-Verlag, New York, 1975) pp 79-100. Review of effect on DNA structure and function: Ch. Zimmer, Prog. Nucleic Acid Res. Mol. Biol. 15, 285-318 (1975).

Abetimus Sodium CAS Registry Number: 169147-32-4

CAS Name: d(C-A-C-A-C-A-C-A-C-A-C-A-C-A-C-A-C-A-C-A)-DNA 5'-ester with 1,2-ethanediylbis(oxy-2,1-ethanediyl) bis[2-(21,21-dihydroxy-21-oxido-4,11-dioxo-20-oxa-13-thia-3,10-diaza-21-phophaheneicos-...
Literature References: B-cell toleragen which prevents the expression of anti-ds-DNA. Consists of four identical ds-DNA oligonucleotides (20 basepairs) attached through a linker to a non-immunogenic modified triethylene glycol base. Relative mass of 54 kDa. Prepn: S. M. Coutts et al., EP 642798; eidem, US 5552391 (1995, 1996 both to La Jolla Pharm.); D. S. Jones et al., J. Med. Chem. 38, 2138 (1995). Clinical evaluation in systemic lupus erythematosus (SLE): R. A. Furie et al., J. Rheumatol. 28, 257 (2001); in prevention of SLE renal flare: D. Alarcon-Segovia et al., Arthritis Rheum. 48, 442 (2003). Review of clinical pharmacology: D. J. Wallace, Expert Opin. Invest. Drugs 10, 111-117 (2001); of clinical experience: M. H. Cardiel, ibid. 14, 77-88 (2005).

Triclabendazole CAS Registry Number: 68786-66-3 三氯苯达唑

CAS Name: 5-Chloro-6-(2,3-dichlorophenoxy)-2-methylthio-1H-benzimidazoleTrademarks: Fasinex (Novartis)
Percent Composition: C 46.75%, H 2.52%, Cl 29.57%, N 7.79%, O 4.45%, S 8.92%
Literature References: Benzimidazole derivative effective against liver fluke. Prepn: J.-J. Gallay et al., BE 865870 corresp to US 4197307 (1978, 1980 both to Ciba-Geigy). Efficacy against immature and mature Fasciola hepatica in sheep, goats: K. Wolff et al., Vet. Parasitol. 13, 145 (1983); in sheep: J. C. Boray et al., Vet. Rec. 113, 315 (1983). Effective also against F. gigantica in sheep: N. Güralp, R. Tinar, J. Helminthol. 58, 113 (1984). Brief review: J. Eckert et al., Biol. Muench. Tieraerztl. Wochenschr. 97, 349 (1984).

Metaclazepam CAS Registry Number: 84031-17-4 7-溴-5-(2-氯苯基)-2,3-二氢-2-(甲氧基甲基)-1-甲基-1H-1,4-苯并二氮杂卓

CAS Name: 7-Bromo-5-(2-chlorophenyl)-2,3-dihydro-2-(methoxymethyl)-1-methyl-1H-1,4-benzodiazepine
Additional Names: brometazepam; metuclazepamPercent Composition: C 54.91%, H 4.61%, Br 20.30%, ...
Literature References: Benzodiazepine deriv with alkoxymethyl group replacing carbonyl in parent compd. Prepn: W. Milkowski et al., DE 2221558; eidem, US 4098786 (1973, 1978 both to Kali-Chemie). Effect on psychomotor performance and memory in volunteers: Z. Subhan, I. Hindmarch, Drugs Exp. Clin. Res. 9, 567 (1983). Interaction with ethanol: H. R. Musch, M. Ruhland, Arzneim.-Forsch. 32, 567 (1982); H. J. Mallach et al., Blutalkohol 20, 196 (1983); V. Schmidt et al., Med. Welt 35, 32 (1984). Clinical studies: G. Laakman et al., Arzneim.-Forsch. 30, 1233 (1980).

Flutoprazepam CAS Registry Number: 25967-29-7 氟托西泮

CAS Name: 7-Chloro-1-(cyclopropylmethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-oneTrademarks: Restar (Sumitomo); Restas (Kanebo)
Percent Composition: C 66.57%, H 4.70%, Cl 10.34...
Literature References: Benzodiazepine derivative. Prepn: H. Yamamoto et al., GB 1253368; eidem, US 3925364 (1971, 1975 both to Sumitomo). New process: T. Okamoto et al., DE 2151540; eidem, US 3832344 (1972, 1974 both to Sumitomo). Stability and degradation mechanism in aqueous solns: K. Akimoto et al., Int. J. Pharm. 3, 109 (1979). Pharmacokinetics and metabolism: A. Kozaki et al., Yakugaku Zasshi 102, 1177 (1982), C.A. 98, 119080q (1983). Pharmacology of flutoprazepam and metabolites: K. Oki et al., Arch. Int. Pharmacodyn. Ther. 269, 180 (1984). Acute toxicity study: H. Takebe et al., Oyo Yakuri 20, 1055 (1980), C.A. 95, 73630b (1981).

Abecarnil CAS Registry Number: 111841-85-1 阿贝卡尔

CAS Name: 4-(Methoxymethyl)-6-(phenylmethoxy)-9H-pyrido[3,4-b]indole-3-carboxylic acid 1-methylethyl ester
Additional Names: isopropyl 6-(benzyloxy)-4-(methoxymethyl)-9H-pyrido[3,4-b]indole-3-c...
Literature References: Benzodiazepine receptor agonist. Prepn: H. Biere et al., DE 3609699 (1987 to Schering AG), C.A. 108, 21872z (1988). Pharmacology and receptor binding studies: D. N. Stephens et al., J. Pharmacol. Exp. Ther. 253, 334 (1990). Determn in biological samples: W. Krause et al., J. Pharm. Sci. 78, 622 (1989). Clinical pharmacokinetics: W. Krause et al., Xenobiotica 21, 763 (1991). Clinical trial in anxiety: J. C. Ballenger et al., Adv. Biochem. Psychopharmacol. 47, 431 (1992). Series of articles on pharmacology, tolerance and clinical evaluation: Psychopharmacol. Ser. 11, 50-147 (1993).

Prucalopride CAS Registry Number: 179474-81-8 普芦卡必利

CAS Name: 4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamideTrademarks: Resolor (J J)
Percent Composition: C 58.77%, H 7.12%, Cl 9.64%, N 11.42%, O 13.0...
Literature References: Benzofuran derivative; specific serotonin 5-HT4 receptor agonist. Prepn: G. H. P. Van Daele et al., WO 9616060; eidem, US 5854260 (1996, 1998 both to Janssen). Effect on isolated gastrointestinal muscle: N. H. Prins et al., Br. J. Pharmacol. 127, 1431 (1999). Clinical stimulation of colonic transit: E. P. Bouras et al., Gut 44, 682 (1999).

Procaine CAS Registry Number: 59-46-1 奴夫卡因

CAS Name: 4-Aminobenzoic acid 2-(diethylamino)ethyl ester
Additional Names: p-aminobenzoyldiethylaminoethanol; 2-diethylaminoethyl p-aminobenzoate
Percent Composition: C 66.07%, H 8.53%, N 1...
Literature References: Benzoic acid derivative with anesthetic activity. Prepn: A. Einhorn, US 812554 (1906); idem, Ann. 371, 125 (1909); A. Einhorn, E. Uhlfelder, ibid. 131. CNS effects: C. G. Peterson, Anesthesiology 16, 976 (1955). Intravenous pharmacokinetics in humans: A. B. Seifen et al., Anesth. Analg. 58, 382 (1979). Clinical evaluation as anti-arrhythmic and cough suppressant during anesthesia: D. S. Thompson et al., Am. J. Surg. 138, 798 (1979). Stabilization of vascular smooth muscle in vitro: K. Kitamura et al., Drugs Exp. Clin. Res. 12, 773 (1986). Toxicity data: W. C. North, K. F. Urbach, J. Am. Pharm. Assoc. Sci. Ed. 45, 382 (1956); E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971).