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

Fungichromin CAS Registry Number: 6834-98-6 喷他霉素

Additional Names: Antibiotic A 246; cogomycin; lagosin; pentamycin
Trademarks: Cantricin (Corvi)
Percent Composition: C 62.66%, H 8.71%, O 28.62%
Literature References: Antifungal polyene macrolide antibiotic, related structurally to filipin, q.v. Isoln from Streptomyces cellulosae: A. A. Tytell et al., Antibiot. Annu. 1954-1955, 716. Isoln (as pentamycin) from S. penticus: S. Umezawa, Y. Tanaka, J. Antibiot. 11A, 26 (1958). Isoln (as lagosin) from S. roseoluteus: C. J. Bessel et al., US 3013947 (1961 to Glaxo). Isoln from S. griseus (FCRC-21): R. C. Pandey et al., Biomed. Mass Spectrom. 7, 93 (1980). Structures: A. C. Cope, H. E. Johnson, J. Am. Chem. Soc. 80, 1504 (1958); A. C. Cope et al., ibid. 84, 2170 (1962); M. L. Dhar et al., J. Chem. Soc. 1964, 842; M. P. Berry, M. C. Whiting, ibid. 862; V. Pozgay et al., J. Antibiot. 29, 472 (1976). Identity of fungichromin with lagosin and cogomycin and comparison of reported physico-chemical constants: R. C. Pandey et al., J. Antibiot. 35, 988 (1982). Biosynthesis and NMR assignment: H. Noguchi et al., J. Am. Chem. Soc. 110, 2938 (1988).

Mycobacillin CAS Registry Number: 18524-67-9

Percent Composition: C 51.08%, H 5.61%, N 11.91%, O 31.40%
Literature References: Antifungal polypeptide antibiotic isolated from culture filtrates of Bacillus subtilis: Majumdar, Bose, Nature 181, 134 (1958). Structural studies: eidem, Biochem. J. 74, 596 (1960); Arch. Biochem. Biophys. 90, 154 (1960). Amino acid configuration: Banerjee, Bose, Nature 200, 471 (1963). Nature of the peptide linkages: Sengupta et al., Biochem. J. 121, 839 (1971). Review: Banerjee et al., Antibiotics vol. II, D. Gottlieb, P. D. Shaw, Eds. (Springer-Verlag, New York, 1967) pp 271-275, 445-446.

Silymarin CAS Registry Number: 65666-07-1 水飞蓟素

Trademarks: Apihepar (Viatris); Laragon (Roemmers); Legalon (Madaus); Pluropon (Boehringer, Ing.); Silarine (Vir); Silepar (Ibirn); Silirex (Lampugnani); Silliver (Abbott); Silmar (Von Boch)
Literature References: Antihepatotoxic principle isolated from the seeds of the milk thistle, Silybum marianum (L.) Gaertn. (Carduus marianus L.). Comprised mainly of three isomers: silidianin, silicristin and the major component, silybin (formerly called silymarin). Characterized as a new class of substances, flavonolignans, almost certainly produced in the plant by a radical coupling of a flavonoid and coniferyl alcohol: Hänsel et al., Dtsch. Apoth. Ztg. 108, 1988 (1968). Isoln and chemistry: Wagner et al., Arzneim.-Forsch. 18, 688 (1968); 24, 466 (1974). Structural work: Janiak, Hänsel, Planta Med. 8, 71 (1960); Hänsel, Schöpflin, Tetrahedron Lett. 1967, 3645; Pelter, Hänsel, ibid. 1968, 2911. Pharmacology and toxicology: Hahn et al., Arzneim.-Forsch. 18, 698 (1968); H. M. Rauen, H. Schriewer, ibid. 23, 148-170 (1973); Halbach, Trost, ibid. 24, 866 (1974).

Sulfametrole CAS Registry Number: 32909-92-5 磺胺美曲

CAS Name: 4-Amino-N-(4-methoxy-1,2,5-thiadiazol-3-yl)benzenesulfonamide
Additional Names: N1-(4-methoxy-1,2,5-thiadiazol-3-yl)sulfanilamide; 3-methoxy-4-(4'-aminobenzenesulfonamido)-1,2,5-thiad...
Literature References: Anti-infective sulfanilamide, related structurally to sulfadiazine, q.v. Prepn: BE 629551 corresp to K. Menzl, US 3247193 (1963, 1966 both to OSSW). Improved prepn: idem, US 4151164 (1979 to Chemie Linz). Bacteriological study (of mixture with trimethoprim): G. Nabert-Bock, H. Grims, Arzneim.-Forsch. 27, 1109 (1977). Tolerance, therapeutic effect, pharmacokinetics: S. Breyer et al., Wien. Med. Wochenschr. 130, 448 (1980). Renal excretion mechanism, pharmacokinetics: T. B. Vree et al., Eur. J. Clin. Pharmacol. 20, 283 (1981). Pharmacokinetics of sulfametrole and its metabolite in man: Y. A. Hester et al., J. Antimicrob. Chemother. 8, 133 (1981). Crystal and molecular structures: C. H. Koo et al., Bull. Korean Chem. Soc. 3, 9 (1982), C.A. 96, 208771 (1982). Single-dose therapy of chancroid with trimethoprim-sulfametrole: F. A. Plummer et al., N. Engl. J. Med. 309, 67 (1983).

Zaltoprofen CAS Registry Number: 74711-43-6 扎托洛芬

CAS Name: 10,11-Dihydro-a-methyl-10-oxodibenzo[b,f]thiepin-2-acetic acid
Additional Names: 2-(10,11-dihydro-10-oxodibenzo[b,f]thiepin-2-yl)propionic acidTrademarks: Soreton (Nippon Chemiphar); ...
Literature References: Anti-inflammatory activity resides in (S)-enantiomer. Prepn: Y. Fujimoto, S. Yamabe, DE 2941869; eidem, US 4247706 (1980, 1981 both to Nippon Chemiphar). Series of articles on pharmacology: Arzneim.-Forsch. 36, 1796-1822 (1986). Resolution of racemate: M. Yamamoto et al., Chirality 2, 280 (1990). HPLC determn in human plasma and urine; pharmacokinetics: J. Oshima et al., J. Chromatogr. 414, 381 (1987).

Terofenamate CAS Registry Number: 29098-15-5 特罗芬那酯

CAS Name: 2-[(2,6-Dichloro-3-methylphenyl)amino]benzoic acid ethoxymethyl ester
Additional Names: N-(2,6-dichloro-m-tolyl)anthranilic acid ethoxymethyl ester; etoclofene
Trademarks: Etofen (...
Literature References: Anti-inflammatory deriv of anthranilic acid, q.v. Prepn: GB 1199386; E. Manghisi, US 3642864 (1970, 1972 both to Lusofarmaco); A. Salembeni et al., Farmaco Ed. Sci. 30, 276 (1975). Biological properties: G. B. Fregnan et al., ibid. 353. Absorption, distribution, excretion: eidem, Boll. Chim. Farm. 114, 85 (1975). Pharmacological and toxicity studies: T. Chieli et al., ibid. 115, 41 (1976).

Bromosaligenin CAS Registry Number: 2316-64-5 5-溴-2-羟基苯甲醇

CAS Name: 5-Bromo-2-hydroxybenzenemethanol
Additional Names: 5-bromo-2-hydroxybenzyl alcohol; 5-bromosaligenin; bromosalizol
Percent Composition: C 41.41%, H 3.48%, Br 39.36%, O 15.76%
Literature References: Anti-inflammatory. Prepd by splitting bromosalicin with emulsin: Visser, Arch. Pharm. 235, 551 (1897); by the action of bromine on saligenin in water: Auwers, Büttner, Ann. 302, 138 (1898); Adams et al., J. Am. Chem. Soc. 45, 2419 (1923); Dunning et al., ibid. 58, 1567 (1936); by the electrolytic reduction of 5-bromo-2-hydroxybenzoic acid: Mettler, Ber. 39, 2939 (1906).

Binifibrate CAS Registry Number: 69047-39-8 比尼贝特

CAS Name: 3-Pyridinecarboxylic acid 2-[2-(4-chlorophenoxy)-2-methyl-1-oxopropoxy]-1,3-propanediyl ester
Additional Names: trihydroxypropane 2-p-chlorophenoxyisobutyrate-1,3-dinicotinate; 2-(p-c...
Literature References: Antilipemic agent structurally related to clofibrate, q.v. Prepn: R. Andreoli, X. Cicera, ES 463218 (1978 to Soc. Espan. Espec. Farm.-Ter.), C.A. 90, 72067h (1979); and pharmacology: eidem, BE 884722 (1980 to Soc. Espan. Espec. Farm.-Ter.). Microhemorheological properties in animals: L. Bruseghini et al., Arzneim.-Forsch. 33, 854 (1983); in patients: M. Dalmau et al., ibid. 858. Clinical evaluation: M. Labios et al., Clin. Hemorheol. Microcirc. 21, 79 (1999).

Xanthatin CAS Registry Number: 26791-73-1 叶黄制菌素

CAS Name: [3aR-(3aa,7b,8ab)]-3,3a,4,7,8,8a-Hexahydro-7-methyl-3-methylene-6-(3-oxo-1-butenyl)-2H-cyclohepta[b]furan-2-one
Percent Composition: C 73.15%, H 7.37%, O 19.49%
Literature References: Antimicrobial agent from Xanthium strumarium L., sens. lat.; X. pennsylvanicum Wallr., Compositae; X. riparium. Isoln: J. E. Little et al., Arch. Biochem. 27, 247 (1950); T. A. Geissman et al., J. Am. Chem. Soc. 76, 685 (1954). Structure: P. G. Deuel, T. A. Geissman, ibid. 79, 3778 (1957). Evaluation as repellent of blue mussel: A. Harada et al., Agric. Biol. Chem. 49, 1887 (1985).

Cyadox CAS Registry Number: 65884-46-0 喹赛多(氰多司)

CAS Name: [(1,4-Dioxido-2-quinoxalinyl)methylene]hydrazide cyanoacetic acid
Additional Names: 2-formylquinoxaline-1,4-dioxide cyanoacetylhydrazone
Percent Composition: C 53.14%, H 3.34%, N 2...
Literature References: Antimicrobial growth-promoting feed additive for poultry, calves and pigs. Growth promoting effects in chickens: J. Broz, B. Sevcik, Biol. Chem. Vyz. Zvirat 13, 357, 375 (1977). Prepn: J. Hebky et al., DE 2829580; eidem, US 4225604 (1979, 1980 both to Spofa). Adsorptive voltammetry determn in plasma: I. Sestáková, M. Kopanica, Talanta 35, 816 (1988). LC determn in animal feeds and gastrointestinal samples: G. J. De Graaf, T. J. Spierenburg, J. Chromatogr. 447, 244 (1988); in goat tissue: Y. Zhang et al., Anal. Sci. 21, 1495 (2005). Heat stability study: idem et al., J. Agric. Food Chem. 53, 9737 (2005). Subchronic toxicity study: G. Fang et al., Food Chem. Toxicol. 44, 36 (2006).