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

Flumecinol CAS Registry Number: 56430-99-0 氟美西诺

CAS Name: a-Ethyl-a-phenyl-3-(trifluoromethyl)benzenemethanol
Additional Names: a-ethyl-3-(trifluoromethyl)benzhydrolTrademarks: Zixoryn (Gedeon Richter); Zyxorin (Gedeon Richter)
Percent Co...
Literature References: Hepatic microsomal enzyme inducer. Prepn: E. Toth et al., DE 2438399; eidem, US 4039589 (1975, 1977 both to Gedeon-Richter). GC determn in biological fluids: I. Klebovich, L. Vereczkey, J. Chromatogr. 221, 403 (1980). Toxicity study: M. Ledniczky et al., Arzneim.-Forsch. 28, 669 (1978). Series of articles on metabolism, CNS effects, enzyme induction, pharmacological properties: ibid. 663-679.

Senecionine CAS Registry Number: 130-01-8 千里光宁

CAS Name: 12-Hydroxysenecionan-11,16-dione
Additional Names: aureine
Percent Composition: C 64.46%, H 7.51%, N 4.18%, O 23.85%
Literature References: Hepatotoxic pyrrolizidine alkaloid from whole plant of Senecio vulgaris L., Compositae and several other Senecio spp. Isoln: Barger, Blackie, J. Chem. Soc. 1936, 743. Structure: Adams, Govindachari, J. Am. Chem. Soc. 71, 1953 (1949); Koekmoer, Warren, J. Chem. Soc. 1955, 63. Conformation: Culvenor, Tetrahedron Lett. 1966, 1091. Toxicity study: P. N. Harris et al., J. Pharmacol. Exp. Ther. 75, 69 (1942). Review of toxicology of senecionine and other pyrrolizidine alkaloids: E. K. McLean, Pharmacol. Rev. 22, 429-483 (1970). Comprehensive reviews of pyrrolizidine alkaloids: L. Bull et al., The Pyrrolizidine Alkaloids (North-Holland, Amsterdam, 1968) 293 pp; F. L. Warren in The Alkaloids vol. 12, R. H. F. Manske, Ed. (Academic Press, New York, 1970) pp 245-331; D. J. Robins, Fortschr. Chem. Org. Naturst. 41, 115-203 (1982).

Lasiocarpine CAS Registry Number: 303-34-4 毛果天芥菜碱

CAS Name: (2Z)-2-Methyl-2-butenoic acid (1S,7aR)-7-[[(2R)-2,3-dihydroxy-2-[(1S)-1-methoxyethyl]-3-methyl-1-oxobutoxy]methyl]-2,3,5,7a-tetrahydro-1H-pyrrolizin-1-yl ester
Percent Composition: C ...
Literature References: Hepatotoxic pyrrolizidine alkaloid isolated from Heliotropium lasiocarpum Fish. et C. Mey. Boraginaceae: G. Menschikoff, Ber. 65, 974 (1932), C.A. 26, 48183 (1932), G. Menschikoff, J. Schdanowitsch, Ber. 69, 1110 (1936), C.A. 30, 52279 (1936). Structure: L. J. Drummond, Nature 167, 41 (1951); R. Adams, B. L. VanDuvren, J. Am. Chem. Soc. 76, 6379 (1954). Review and evaluation of studies of carcinogenicity and toxicity in laboratory animals: IARC Monographs 10, 281-290, 333-342 (1976). Comprehensive reviews: L. Bull et al., The Pyrrolizidine Alkaloids (North-Holland, Amsterdam, 1965) 293 pp; F. L. Warren in The Alkaloids vol. 12, R. H. F. Manske, Ed. (Academic Press, New York, 1970) pp 245-331; D. J. Robins, Fortschr. Chem. Org. Naturst. 41, 115-203 (1982).

Heliosupine CAS Registry Number: 32728-78-2 [7-[(Z)-2-甲基丁-2-烯酰基]氧基-5,6,7,8-四氢-3H-吡咯里嗪-1-基]甲基2,3-二羟基-2-(1-羟基乙基)-3-甲基丁酸酯

CAS Name: 2-Methyl-2-butenoic acid 7-[[2,3-dihydroxy-2-(1-hydroxyethyl)-3-methyl-1-oxobutoxy]methyl]-2,3,5,7a-tetrahydro-1H-pyrrolizin-1-yl ester
Additional Names: cynoglossophine
Percent Co...
Literature References: Hepatotoxic pyrrolizidine alkaloid isolated from Heliotropium supinum L., Boraginaceae: Denisova et al., Dokl. Akad. Nauk SSSR 93, 59 (1953); from Cynoglossum officinale L., Boraginaceae: Man'ko, Borisyuk, Ukr. Khim. Zh. 23, 362 (1957), C.A. 52, 2188a (1958); Man'ko, Marchenko, Khim. Prir. Soedin. 7, 537 (1971), C.A. 75, 126598t (1971). Identity with cynoglossophine: Man'ko, Ukr. Khim. Zh. 25, 627 (1959), C.A. 54, 12494d (1960). Structure: Crowley, Culvenor, Aust. J. Chem. 12, 694 (1959). Biosynthesis studies: Crout, J. Chem. Soc. C 1967, 1233. Reviews: see Lasiocarpine.

Seneciphylline CAS Registry Number: 480-81-9 千里光菲灵碱

CAS Name: 13,19-Didehydro-12-hydroxysenecionan-11,16-dione
Additional Names: jacodine; a-longilobine
Percent Composition: C 64.85%, H 6.95%, N 4.20%, O 24.00%
Literature References: Hepatotoxic pyrrolizidine alkaloid, common constituent of Senecio species. Isoln from Senecio platyphllus DC. Compositae: A. Orechoff, W. Tiedebel, Ber. 68, 650 (1935); from S. jacobaea L.: G. Barger, J. J. Blackie, J. Chem. Soc. 1937, 584; from Crotalaria juncea L. Leguminosae: R. Adams, M. Gianturco, J. Am. Chem. Soc. 78, 1919 (1956). Identity with a-longilobine: R. Adams, J. H. Looker, ibid. 73, 134 (1951). Identity with jacodine: R. B. Bradbury, C. C. J. Culvenor, Chem. Ind. (London) 1954, 1021. Structural study: R. Adams et al., J. Am. Chem. Soc. 74, 700 (1952). Revised structure: S. Masume, Chem. Ind. (London) 1959, 21. Review and evaluation of toxicity and carcinogenicity studies: IARC Monographs 10, 319-325, 333-342 (1976). Comprehensive reviews of seneciphylline and other pyrrolizidine alkaloids: L. Bull et al., The Pyrrolizidine Alkaloids (North-Holland, Amsterdam, 1968) 293 pp; F. L.Warren in The Alkaloids vol. 12, R. H. F. Manske, Ed. (Academic Press, New York, 1970) pp 245-331.

Retrorsine CAS Registry Number: 480-54-6 倒千里光碱

CAS Name: 12,18-Dihydroxysenecionan-11,16-dione
Additional Names: b-longilobine
Percent Composition: C 61.52%, H 7.17%, N 3.99%, O 27.32%
Literature References: Hepatotoxic pyrrolizidine alkaloid; common constituent of Senecio species. Isoln from Senecio retrorsus DC, Compositae: R. H. F. Manske, Can. J. Chem. 5, 651 (1931); G. Barger et al., J. Chem. Soc. 1935, 11; from Crotalaria usaramoensis E. G. Baker, Leguminosae: C. C. J. Culvenor, L. W. Smith, Aust. J. Chem. 19, 2127 (1966). Structure: S. M. H. Christie et al., J. Chem. Soc. 1949, 1700; E. C. Leisegang, F. L. Warren, ibid. 1950, 702. Identity with b-longilobine: F. L. Warren et al., J. Am. Chem. Soc. 72, 1421 (1950). Review and evaluation of toxicity and carcinogenicity studies: IARC Monographs 10, 303-312, 333-342 (1976). Comprehensive reviews of pyrrolizidine alkaloids: L. B. Bull et al., The Pyrrolizidine Alkaloids (North Holland, Amsterdam, 1968) 293 pp; F. L. Warren in The Alkaloids vol. 12, R. H. F. Manske, Ed. (Academic Press, New York, 1970) pp 245-331.

Hachimycin CAS Registry Number: 1394-02-1 曲古霉素

CAS Name: Trichomycin
Trademarks: Trichonat (Grñenthal)
Literature References: Heptaene macrolide antibiotic substance produced by Streptomyces hachijoensis from soil of the Pacific Island Hachijo Jima: S. Hosoya et al., J. Antibiot. 5, 564 (1952); T. Yamaguchi, ibid. 7A, 10 (1954). Purification and prepn of insol derivs: S. Hosoya et al., ibid. 8A, 5 (1955). At one time, trichomycin was believed to be identical to candicidin and hamycin, q.q.v.: H. Burrows, D. Calam, J. Chromatogr. 53, 566 (1970). Subsequent HPLC studies have shown the three polyene antibiotics to be different entities: P. Helboe et al., ibid. 189, 249 (1980). Active against Trichomonas vaginalis, Treponema pallidum, Trichophyton, Candida, and yeast, weak activity against Aspergillus and Penicillium: T. Yamaguchi, J. Antibiot. 7A, 10 (1954). Toxicity: S. Hosoya et al., J. Antibiot. 6A, 98 (1953). Review: S. A. Waksman, H. A. Lechevalier, The Actinomycetes vol. III (Williams Wilkins, Baltimore, 1962) pp 397-399.

Candicidin CAS Registry Number: 1403-17-4 杀念菌素

Additional Names: Levorin
Trademarks: Vanobid
Literature References: Heptaene macrolide antifungal antibiotic complex composed of candicidins A, B, C and D (major component). Produced by a strain of Streptomyces griseus (Rutgers no. 3570): Lechevalier et al., Mycologia 45, 155 (1953). Methods of isoln: Siminoff, US 2872373 (1959 to Penick); Waksman, Lechevalier, US 2992162 (1961 to Rutgers Res. Ed. Found.). Activity: Kligman, Lewis, Proc. Soc. Exp. Biol. Med. 82, 399 (1953); Lancet 1, 507 (1954); Lechevalier, Presse Med. 61, 1327 (1953). Structure of candicidin D: J. Zielinski et al., Tetrahedron Lett. 1979, 1791. Biosynthesis studies: Liu et al., J. Antibiot. 25, 116 (1972). Anticholesteremic property and mode of action studies: I. H. Kwon, H. Fisher, Nutr. Rep. Int. 9, 245 (1974); A. K. Singhal et al., Lipids 16, 423 (1981). HPLC comparison of candicidin, hamycin, trichomycin, q.q.v.: P. Helboe et al., J. Chromatogr. 189, 249 (1980). Toxicity study: L. C. Vining et al., Antibiot. Annu. 1954-55, 980.

Zinc Selenate CAS Registry Number: 13597-54-1 五水合硒酸锌

Percent Composition: O 30.71%, Se 37.89%, Zn 31.39%
Literature References: Heptahydrate prepd by the action of selenic acid on zinc carbonate: Banks, J. Chem. Soc. 1934, 1010.

Nitisinone CAS Registry Number: 104206-65-7 尼替西农

CAS Name: 2-[2-Nitro-4-(trifluoromethyl)benzoyl]-1,3-cyclohexanedione
Additional Names: NTBC
Trademarks: Orfadin (Swedish Orphan )
Percent Composition: C 51.07%, H 3.06%, F 17.31%, N 4.25...
Literature References: Herbicidal triketone that inhibits 4-hydroxyphenylpyruvate dioxygenase (HPPD), an enzyme involved in plastoquinone biosynthesis in plants and in tyrosine catabolism in mammals. Prepn: C. G. Carter, EP 186118 (1986 to Stauffer); idem, US 5006158 (1991 to ICI). Inhibition of HPPD in plants: M. P. Prisbylla et al., Brighton Crop Prot. Conf. - Weeds 1993, 731; in rats: M. K. Ellis et al., Toxicol. Appl. Pharmacol. 133, 12 (1995). LC determn in plasma: M. Bielenstein et al., J. Chromatogr. B 730, 177 (1999). Clinical evaluation in hereditary tyrosinemia type I: S. Lindstedt et al., Lancet 340, 813 (1992). Review of toxicology and therapeutic development: E. A. Lock et al, J. Inherited Metab. Dis. 21, 498-506 (1998); of clinical experience: E. Holme, S. Lindstedt, ibid. 507-517.