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

Tolonidine CAS Registry Number: 4201-22-3 托洛尼定

CAS Name: N-(2-Chloro-4-methylphenyl)-4,5-dihydro-1H-imidazol-2-amine
Additional Names: 2-(2-chloro-p-toluidino)-2-imidazoline; 2-(2-chloro-4-methylphenyl)amino-1,3-diazacyclopentene-2
Perce...
Literature References: Orally active antihypertensive agent, related structurally to clonidine. Prepn: NL 6411516; US 3236857; US 6411516; US 3454701 (1965, 1966, 1969 all to Boehringer, Ing.). Synthesis and hypotensive activity: P. B. M. Timmermans et al., Rec. Trav. Chim. 97, 51 (1978). Pharmacological properties: C. Cosnier et al., Arzneim.-Forsch. 25, 1557, 1802, 1926 (1975). Structure-activity study: P. B. M. Timmermans, P.A. Van Zwieten, J. Med. Chem. 20, 1636 (1977). Chromatographic study: P. B. M. Timmermans et al., J. Chromatogr. 144, 215 (1977). Quantum chemical studies: eidem, Arzneim.-Forsch. 27, 2266 (1977). Radioimmunoassay disposition study: B. Jarrott, S. Spector, J. Pharmacol. Exp. Ther. 207, 195 (1978). Toxicity study: D. Cosnier et al., Arzneim.-Forsch. 25, 1926 (1975).

Itraconazole CAS Registry Number: 84625-61-6 伊曲康唑

CAS Name: 4-[4-[4-[4-[[2-(2,4-Dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-2,4-dihydro-2-(1-methylpropyl)-3H-1,2,4-triazol-3-one
Addit...
Literature References: Orally active antimycotic structurally related to ketoconazole, q.v. Prepn: J. Heeres, L. J. J. Backx, EP 6711; eidem, US 4267179 (1980, 1981 both to Janssen); J. Heeres et al., J. Med. Chem. 27, 894 (1984). In vitro activity: A. Espinel-Ingroff et al., Antimicrob. Agents Chemother. 26, 5 (1984). HPLC determn in biological samples: R. Woestenborghs et al., J. Chromatogr. 413, 332 (1987). Symposium on pharmacology and clinical efficacy: Rev. Infect. Dis. 9, Suppl 1, S1-S152 (1987). Toxicity data: H. Van Cauteren et al., ibid. S43. Review of clinical pharmacokinetics: J. Heykants et al., Mycoses 32, Suppl 1, 67-87 (1989); of clinical efficacy in dermatophytosis: P. De Doncker, G. Cauwenbergh, Br. J. Clin. Pract. Suppl. 71, 118-122 (1990). Review: A. M. Sugar, Curr. Clin. Top. Infect. Dis. 13, 74-98 (1993).

Bifluranol CAS Registry Number: 34633-34-6

CAS Name: rel-4,4'-[(1R,2S)-1-Ethyl-2-methyl-1,2-ethanediyl]bis[2-fluorophenol]
Additional Names: erythro-3,3'-difluoro-4,4'-dihydroxy-a-ethyl-a'-methyldibenzylTrademarks: Prostarex (Biorex) Literature References: Orally active antiprostatic agent. Prepn: J. C. Turner, R. P. Chan, DE 2110428; eidem, US 4051263 (1971, 1977 both to Biorex). Antiprostatic activity: J. B. Dekanski, Br. J. Pharmacol. 71, 11 (1980). Chemistry, disposition in animals: D. J. Pope et al., J. Pharm. Pharmacol. 33, 297 (1981). Metabolism: eidem, ibid. 302.

Sorivudine CAS Registry Number: 77181-69-2 索立夫定

CAS Name: 1-b-D-Arabinofuranosyl-5-[(1E)-2-bromoethenyl]-2,4(1H,3H)-pyrimidinedione
Additional Names: 1-b-D-arabinofuranosyl-(E)-5-(2-bromovinyl)uracil; 5-bromovinyl-araU; brovavir; BV-araU; BV...
Literature References: Orally active antiviral agent; inhibits viral DNA synthesis. Prepn: H. Machida, S. Sakata, EP 31128; eidem, US 4386076 (1981, 1983 both to Yamassa Shoyu); S. Sakata et al., Nucleic Acids Symp. Ser. 8, s39 (1980); R. Busson et al., ibid. 9, 49 (1981). Antiviral activity and toxicity: H. Machida, S. Sakata, Antiviral Res. 4, 135 (1984). Mechanism of action studies: T. Yokota et al., Mol. Pharmacol. 36, 312 (1989); H. Machida, Adv. Exp. Med. Biol. 278, 255 (1990). Clinical trial in herpes zoster infection: M. Niimura, ibid. 267.

Mabuterol CAS Registry Number: 56341-08-3 马布台诺

CAS Name: 4-Amino-3-chloro-a-[[(1,1-dimethylethyl)amino]methyl]-5-(trifluoromethyl)benzenemethanol
Additional Names: 4-amino-a-[(tert-butylamino)methyl]-3-chloro-5-(trifluoromethyl)benzyl alcoh...
Literature References: Orally active b2-adrenergic agonist related to clenbuterol, q.v. Prepn and resolution of isomers: BE 808743 (1974 to Thomae); G. Engelhardt et al., US 4119710 (1978 to Boehringer Ing.); eidem, Arzneim.-Forsch. 34, 1612 (1984). Series of articles on pharmacology, pharmacokinetics, toxicology and clinical studies: ibid. 1625-1700. Toxicity data: K. Amemiya et al., ibid., 1680. Teratological study: A. M. Hoberman et al., J. Am. Coll. Toxicol. 4, 91 (1985). Determn in human urine and plasma by enzyme immunoassay: I. Yamamoto et al., J. Immunoassay 6, 261 (1985).

Cefroxadine CAS Registry Number: 51762-05-1 头孢沙定

CAS Name: (6R,7R)-7-[[(2R)-Amino-1,4-cyclohexadien-1-ylacetyl]amino]-3-methoxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: 7-[D-2-amino-2-(1,4-cyclohexadienyl)...
Literature References: Orally active cephalosporin deriv. Prepn: R. Scartazzini, H. Bickel, DE 2331133; eidem, US 4073902 (1974, 1978 both to Ciba-Geigy). Antibiotic activity: O. Zak et al., J. Antibiot. 29, 653 (1976). In vivo and in vitro microbiological evaluation: K. Yasuda et al., Antimicrob. Agents Chemother. 18, 105 (1980). Pharmacokinetics: T. Bergan, Chemotherapy 26, 225 (1980). Series of articles on activity, toxicity, reproduction studies: Chemotherapy (Tokyo) 28, Suppl 3, 1-335 (1980).

Carmofur CAS Registry Number: 61422-45-5 氟脲己胺

CAS Name: 5-Fluoro-N-hexyl-3,4-dihydro-2,4-dioxo-1(2H)-pyrimidinecarboxamide
Additional Names: 1-(n-hexylcarbamoyl)-5-fluorouracil; HCFU
Trademarks: Mifurol (Mitsui); Yamaful (Yamanouchi) Literature References: Orally active cytostatic deriv of fluorouracil, q.v. Prepn: S. Ozaki et al., JP Kokai 77 78886, C.A. 87, 152265 (1977); eidem, US 4071519 (1977, 1978 both to Mitsui); eidem, Bull. Chem. Soc. Jpn. 50, 2406 (1977). Anti-tumor activity: A. Hoshi et al., Chem. Pharm. Bull. 26, 161 (1978). Determn in body fluids: S. Watanabe et al., Chemotherapy (Tokyo) 27, 778 (1979); O. Nakajima et al., J. Chromatogr. 225, 91 (1981). General pharmacology: Z. Henmi et al., Oyo Yakuri 19, 369 (1980), C.A. 93, 125639s (1980). Pharmacokinetics: M. Iigo et al., Cancer Chemother. Pharmacol. 4, 189 (1980). Metabolism: eidem, Xenobiotica 10, 847 (1980); T. Kobari et al., ibid. 11, 57 (1981). Phase I clinical study: Y. Koyama, Y. Koyama, Cancer Treat. Rep. 64, 861 (1980). Mutagenicity study: Y. Seino et al., Cancer Res. 38, 2148 (1978). Review: T. Taguchi, Recent Results Cancer Res. 70, 125-132 (1980).

Capecitabine CAS Registry Number: 154361-50-9 卡培他滨

CAS Name: 5'-Deoxy-5-fluoro-N-[(pentyloxy)carbonyl]cytidine
Additional Names: [1-(5-deoxy-b-D-ribofuranosyl)-5-fluoro-1,2-dihydro-2-oxo-4-pyrimidinyl]carbamic acid pentyl ester; pentyl 1-(5-deo...
Literature References: Orally active fluoropyrimidine. Prodrug of doxifluridine, q.v., designed to be metabolized to 5-fluorouracil, q.v., at the tumor site. Prepn: M. Arasaki et al., EP 602454; eidem, US 5472949 (1994, 1995 both to Hoffmann-La Roche). Metabolism by tumor enzymes: T. Ishikawa et al., Cancer Res. 58, 685 (1998). Clinical comparison with i.v. fluorouracil in colorectal cancer: P. M. Hoff et al., J. Clin. Oncol. 19, 2282 (2001); E. Van Cutsem et al., ibid. 4097. Review of pharmacology and clinical experience: J. K. McGavin, K. L. Goa, Drugs 61, 2309-2326 (2001).

Gestodene CAS Registry Number: 60282-87-3 孕二烯酮

CAS Name: (17a)-13-Ethyl-17-hydroxy-18,19-dinorpregna-4,15-dien-20-yn-3-one
Additional Names: 17a-ethynyl-17b-hydroxy-18-methyl-4,15-estradien-3-one; 17a-ethynyl-13-ethyl-17b-hydroxy-4,15-gonad...
Literature References: Orally active gestogen with progesterone-like profile of activity. Prepn: BE 847090; H. Hofmeister et al., US 4081537 (1977, 1978 both to Schering AG). Pharmacokinetics: B. Duesterberg et al., Contraception 24, 673 (1981); B. Duesterberg, Steroids 43, 43 (1984). Comparative study of anti-aldosterone activity: W. Losert et al., Arzneim.-Forsch. 35, 459 (1985). Clinical trial as oral contraceptive: G. Hoppe, Adv. Contracept. 3, 159 (1987).

Azelastine CAS Registry Number: 58581-89-8 盐酸氮卓斯汀

CAS Name: 4-[(4-Chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone
Additional Names: 4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone; 4-...
Literature References: Orally active H1-histamine receptor antagonist. Prepn: BE 778269; D. Vogelsang et al., US 3813384 (1972, 1974 both to Asta-Werke AG). Synthesis and x-ray structure determn: G. Scheffler et al., Arch. Pharm. 321, 205 (1988). Pharmacology: K. Tasaka, M. Akagi, Arzneim.-Forsch. 29, 488 (1979). Pharmacology and toxicology: H. J. Zechel et al., ibid. 31, 1184 (1981). Series of articles on pharmacokinetics, pharmacology and toxicology: ibid. 1184-1238. Mechanism of action studies: N. Chand et al., Int. J. Immunopharmacol. 7, 833 (1985); eidem, Br. J. Pharmacol. 87, 443 (1986). HPLC determn in plasma: J. Pivonka et al., J. Chromatogr. 420, 89 (1987). Clinical evaluations in asthma: H. Magnussen, Chest 91, 855 (1987); M. K. Albazzaz, K. R. Patel, Thorax 43, 306 (1988); in allergic conjunctivitis: G. W. Canonica et al., Curr. Med. Res. Opin. 19, 321-329 (2003).