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

Enduracidin CAS Registry Number: 11115-82-5 恩拉霉素

Additional Names: Enramycin
Literature References: Cyclodepsipeptide antibiotic produced by Streptomyces fungicidicus, strain no. B5477, from a soil sample collected in Nishinomiya, Hyogo Prefecture, Japan: Higashide et al., J. Antibiot. 21, 126 (1968). Originally thought to be a single compound. Isoln and characterization: Asai et al., ibid. 138; FR 1514139; GB 1163270 (1968, 1969 to Takeda). Manufacturing process: JP Kokai 82 79896 (1982 to Takeda), C.A. 97, 108525s (1982). Separation into two components, enduracidins A and B: Hori et al., Chem. Pharm. Bull. 21, 1171 (1973). The two components are each composed of seventeen amino acids, sixteen of which form a macrocyclic peptide lactone, and only differ by one methylene group in their fatty acid moieties. Structural studies: Hori et al., ibid. 1175. Final structure: Iwasaki et al., ibid. 1184. Antibacterial activity: Goto et al., J. Antibiot. 21, 119 (1968); Tsuchiya et al., ibid. 147; M. Kawakami et al., ibid. 24, 583 (1971). Toxicology: H. Yokotani et al., Takeda Kenkyusho Nempo 28, 76 (1969), C.A. 72, 77300s (1970).

Valinomycin CAS Registry Number: 2001-95-8 缬氨霉素

Percent Composition: C 58.36%, H 8.16%, N 7.56%, O 25.91%
Literature References: Cyclododecadepsipeptide ionophore antibiotic produced by Streptomyces fulvissimus and related to the enniatins, q.v. Composed of 3 moles each of L-valine, D-a-hydroxyisovaleric acid, D-valine, and L-lactic acid linked alternately to form a 36-membered ring: Brockmann et al., Ber. 88, 57 (1955); Ann. 603, 216 (1957). Structural studies: Shemyakin et al., Tetrahedron Lett. 1963, 351; Tetrahedron 19, 995 (1963). Proposed structure: Brockmann et al., Naturwissenschaften 50, 689 (1963). Structure and synthesis: Shemyakin et al., Tetrahedron Lett. 1963, 1921. Solid phase synthesis: Gisin et al., J. Am. Chem. Soc. 91, 2691 (1969); Losse, Klengel, Tetrahedron 27, 1423 (1971). Biosynthesis: Smirnova et al., C.A. 73, 97347m (1970); Ristow et al., FEBS Lett. 42, 127 (1974). Conformation: Ivanov et al., Biochem. Biophys. Res. Commun. 34, 803 (1969); Onishi, Urry, ibid. 36, 194 (1969); Duax et al., Science 176, 911 (1972). Review: Y. A. Ovchinnokov, V. T. Ivanov, "The Cyclic Peptides: Structure, Conformation, and Function", in The Proteins vol. V, H. Neurath, R. L. Hill, Eds. (Academic Press, New York, 3rd ed., 1982) pp 563-573.

Pamicogrel CAS Registry Number: 101001-34-7

CAS Name: 2-[4,5-Bis(4-methoxyphenyl)-2-thiazolyl]-1H-pyrrole-1-acetic acid ethyl ester
Additional Names: ethyl 2-[4,5-bis(p-methoxyphenyl)-2-thiazolyl]pyrrole-1-acetatePercent Composition: C 6...
Literature References: Cyclooxygenase inhibitor. Prepn: K. Yoshino et al., EP 159677; eidem, US 4659726 (1985, 1987 both to Kanebo). HPLC determn in plasma and urine: Y. Nakada et al., Chem. Pharm. Bull. 38, 1093 (1990). Pharmacokinetics: Y. Nakada et al., Yakuzaigaku 53, 210 (1993), C.A. 120, 315100 (1993). Activity as antithrombotic: K. Yokoto et al., Jpn. J. Pharmacol. 68, 201 (1995); as platelet aggregation inhibitor: K. Yokoto et al., J. Pharm. Pharmacol. 47, 768 (1995). Evaluation of cerebral protective effects: N. Yamamoto et al., Jpn. J. Pharmacol. 69, 421 (1995); eidem, Eur. J. Pharmacol. 297, 225 (1996).

Flunixin CAS Registry Number: 38677-85-9 氟尼辛葡甲胺

CAS Name: 2-[[2-Methyl-3-(trifluoromethyl)phenyl]amino]-3-pyridinecarboxylic acid
Additional Names: 2-(2-methyl-3-trifluoromethylanilino)nicotinic acid; 2-(a3,a3,a3-trifluoro-2,3-xylidino)nicot...
Literature References: Cyclooxygenase inhibitor. Prepn: M. H. Sherlock, N. Sperber, BE 679271; eidem, US 3337570 (1966, 1967 both to Schering). Prepn of the acid and meglumine salt: M. H. Sherlock, BE 812772; idem, US 3839344 (both 1974 to Schering). Pharmacodynamics in horses: M. M. Hardee, J. N. Moore, Res. Vet. Sci. 40, 152 (1986); and pharmacokinetics: L. R. Soma et al., J. Vet. Pharmacol. Ther. 15, 292 (1992). GC determn in urine: M. Johansson, E. -L. Anlér, J. Chromatogr. 427, 55 (1988). Clinical evaluation in horses: J. W. Houdeshell, P. W. Hennessey, J. Equine Med. Surg. 1, 57 (1977). Experimental use in food-producing animals: M. Kopcha, A. S. Ahl, J. Am. Vet. Med. Assoc. 194, 45 (1989). Comparative toxicological study in horses: C. G. MacAllister et al., ibid. 202, 71 (1993).

Lornoxicam CAS Registry Number: 70374-39-9 氯诺昔康

CAS Name: 6-Chloro-4-hydroxy-2-methyl-N-2-pyridinyl-2H-thieno[2,3-e]-1,2-thiazine-3-carboxamide 1,1-dioxide
Additional Names: 6-chloro-4-hydroxy-2-methyl-3-(2-pyridylcarbamoyl)-2H-thieno[2,3-e]...
Literature References: Cyclooxygenase inhibitor; structurally similar to tenoxicam, q.v. Prepn: R. Pfister et al., DE 2838851; eidem, US 4180662 (both 1979 to Hoffmann-La Roche). Clinical pharmacokinetics: S. I. Ankier et al., Postgrad. Med. J. 64, 752 (1988). Symposium on pharmacology and clinical experience: ibid. 66, Suppl. 4, S1-S50 (1990). Overview of pharmacology and safety assessment: T. P. Pruss et al., ibid. S18.

Suriclone CAS Registry Number: 53813-83-5 舒立克隆

CAS Name: 4-Methyl-1-piperazinecarboxylic acid 6-(7-chloro-1,8-naphthyridin-2-yl)-2,3,6,7-tetrahydro-7-oxo-5H-1,4-dithiino[2,3-c]pyrrol-5-yl ester
Additional Names: 6-(7-chloro-1,8-naphthyridin...
Literature References: Cyclopyrrolone derivative; structural analog of zopiclone. Prepn: C. Jeanmart et al., DE 2360362; eidem, US 3948917 (1974, 1976 both to Rhone-Poulenc). Benzodiazepine receptor binding studies: J.-C. Blanchard, L. Julou, J. Neurochem. 40, 601 (1983); R. R. Trifiletti, S. H. Snyder, Mol. Pharmacol. 26, 458 (1984); J. L. Zundel et al., Life Sci. 36, 2247 (1985). Pharmacology: L. Julou et al., Pharmacol. Biochem. Behav. 23, 653 (1985). Clinical evaluation as an anxiolytic: Y. D. Lapierre, K. L. Oyewumi, Prog. Neuro-Psychopharmacol. Biol. Psychiatry 7, 805 (1983); W. E. Falk et al., Psychopharmacol. Bull. 23, 134 (1987).

L -2-Oxo-4-thiazolidinecarboxylic acid CAS Registry Number: 19771-63-2 L-2-噻唑林二酮-4-甲酸

CAS Name: (4R)-2-Oxo-4-thiazolidinecarboxylic acid
Additional Names: OTCA; OTC
Trademarks: Procysteine (Baxter)
Percent Composition: C 32.65%, H 3.42%, N 9.52%, O 32.62%, S 21.79%
Literature References: Cysteine prodrug. Prepn: J. A. Maclaren, Aust. J. Chem. 21, 1891 (1968); T. Kömives, Org. Prep. Proced. Int. 21, 251 (1989). Crystal structure: N. Ramasubbu, R. Parthasarathy, Int. J. Pept. Protein Res. 34, 153 (1989). Precursor for cysteine and use as glutathione biosynthesis stimulant: J. M. Williamson et al., Proc. Natl. Acad. Sci. USA 79, 6246 (1982); in chicks: T. K. Chung et al., J. Nutr. 120, 158 (1990). Toxicity: R. D. White et al., Acute Toxic. Data 1, 164 (1992); R. D. White et al., Toxicol. Lett. 69, 15 (1993). Clinical evaluation in HIV infection: G. Giorgi et al., Curr. Ther. Res. 52, 461 (1992); in asymptomatic HIV infection: R. C. Kalayjian et al., J. Acquired Immune Defic. Syndr. 7, 369 (1994). HPLC determn in plasma: L. W. Webb et al., J. Chromatogr. B 654, 257 (1994).

Zafirlukast CAS Registry Number: 107753-78-6 扎鲁司特

CAS Name: [3-[[2-Methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]carbamic acid cyclopentyl ester
Additional Names: cyclopentyl 3-[2-methoxy-4-[(o-toly...
Literature References: Cysteinyl leukotriene type 1 receptor antagonist. Prepn: F. J. Brown et al., EP 199543; P. R. Bernstein et al., US 4859692 (1986, 1989 both to ICI); V. G. Matassa et al., J. Med. Chem. 33, 1781 (1990). Improved prepn: K. Srinivas et al., Org. Process Res. Dev. 8, 952 (2004). Preclinical pharmacology: R. D. Krell et al., Am. Rev. Respir. Dis. 141, 978 (1990). Effect on allergen-induced bronchoconstriction: S. R. Findlay et al., J. Allergy Clin. Immunol. 89, 1040 (1992); K. M. O'Shaughnessy et al., Am. Rev. Respir. Dis. 147, 1431 (1993). Review of pharmacology and clinical efficacy in asthma: C. J. Dunn, K. L. Goa, Drugs 61, 285-315 (2001); of clinical pharmacokinetics: P. N. R. Dekhuijzen, P. P. Koopmans, Clin. Pharmacokinet. 41, 105-114 (2002).

Misoprostol CAS Registry Number: 59122-46-2 米索前列醇

CAS Name: (11a,13E)-11,16-Dihydroxy-16-methyl-9-oxoprost-13-en-1-oic acid methyl ester
Additional Names: (±)-methyl-(1R,2R,3R)-3-hydroxy-2-[(E)-(4RS)-4-hydroxy-4-methyl-1-octenyl]-5-oxocyc...
Literature References: Cytoprotective prostaglandin PGE1 analog; also exhibits uterotonic and cervical-ripening actions. Double racemate comprised of the (+)- and (-)-enantiomers of the 16R- and 16S-forms. The pharmacologically active form is the (11R,16S)-enantiomer. Prepn: P. W. Collins, R. Pappo, BE 827127; eidem, US 3965143 (1975, 1976 both to Searle); P. W. Collins et al., Tetrahedron Lett. 48, 4217 (1975). Prepn, activity, NMR data: P. Collins et al., J. Med. Chem. 20, 1152 (1977). HPLC resolution of enantiomers: D. A. Roston, R. Wijayaratne, Anal. Chem. 60, 948 (1988). Mechanism of gastric secretory inhibition: D. G. Colton et al., Arch. Int. Pharmacodyn. Ther. 236, 86 (1978). Symposium on pharmacology and clinical efficacy: Dig. Dis. Sci. 30, Suppl. 11, 114S-205S (1985). Toxicity data: F. N. Kotsonis et al., ibid. 142S. Clinical trial in prevention of NSAID-induced ulcer: D. Y. Graham et al., Ann. Intern. Med. 119, 257 (1993); to induce labor: H. Fletcher et al., Obstet. Gynecol. 83, 244 (1994). Review of clinical experience in pregnancy: A. B. Goldberg et al., N. Engl. J. Med. 344, 38-47 (2001).

Colloidal Bismuth Subcitrate CAS Registry Number: 57644-54-9 枸橼酸铋钾

Additional Names: CBS
Trademarks: De-Nol (Yamanouchi); De-Noltab (Yamanouchi); Duosol (Interdelta); Ulcerone (Yamanouchi)
Literature References: Cytoprotective, polymeric bismuth citrato complex; also known as tripotassium dicitrato bismuthate. General prepn of colloidal bismuth solution: L. Vanino, cited in Mellor's vol. IX, 598 (1929). Manufacturing processes: C. J. McLoughlin, R. B. Himstedt, DE 2501787; P. J. H. Bos et al., EP 75992; eidem, US 4801608 (1975, 1985, 1989 all to Gist-Brocades). Analytical study: D. R. Williams, J. Inorg. Nucl. Chem. 39, 711 (1977). Crystal structure: E. Asato et al., Chem. Lett. 1992, 1967. Pharmacology: J. Wieriks et al., Scand. J. Gastroenterol. 17, Suppl. 80, 11 (1982). Modes of action: D. W. R. Hall, ibid. 24, Suppl. 157, 3 (1989); S. P. Lee, ibid. 26, Suppl. 185, 1 (1991). Pharmacokinetics and safety: L. Z. Benet ibid. 29. Symposia on pharmacology and clinical efficacy: ibid. 21, Suppl. 122, 1-54 (1986); Digestion 37, Suppl. 2, 1-64 (1987). Clinical trials in Helicobacter pylori associated gastritis and ulcer: T. Rokkas et al., Gut 29, 1386 (1988); W. A. de Boer et al., Am. J. Gastroenterol. 89, 1993 (1994).