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

Trichosanthin CAS Registry Number: 60318-52-7

Trademarks: GLQ223 (Genelabs)
Literature References: Active component of the traditional Chinese medicine, Tian Hua Fen (Radix Trichosanthis), known since 300 A.D. and used in gynecological disorders and abortion. Basic polypeptide of 234 amino acids, Mr 26,000 Da, isolated from the roots of Trichosanthes kirilowii Maxim, Cucurbitaceae. Purification, characterization, and amino acid sequence: W. Yu et al., Pure Appl. Chem. 58, 789 (1986); J. M. Maraganore et al., J. Biol. Chem. 262, 11628 (1987). Conformation: S. Kubota et al., Biochim. Biophys. Acta 871, 101 (1986); and homology with ricin, q.v.: eidem, Int. J. Pept. Protein Res. 30, 646 (1987). Inhibition of protein synthesis: H. W. Yeung et al., ibid. 31, 265 (1988). Inhibition of HIV replication: M. S. McGrath et al., Proc. Natl. Acad. Sci. USA 86, 2844 (1989). Abortifacient activity in animals: M. C. Chang et al., Contraception 19, 175 (1979); S. K. Saksena et al., ibid. 20, 367 (1979); I. F. Lau et al., ibid. 21, 77 (1980). Clinical trial as abortifacient: K. F. Cheng, Obstet. Gynecol. 59, 494 (1982).

Ferumoxides CAS Registry Number: 119683-68-0

Trademarks: Feridex (Advanced Magnetics); Endorem (Guerbet)
Literature References: Active ingredient of colloidal super paramagnetic iron oxide (SPIO) consisting of nonstoichiometric magnetite cores coated with dextran. Designed for use as hepatic MRI contrast agent. Prepn: E. V. Groman, L. Josephson, WO 8800060; eidem, US 4770183 (both 1988 to Advanced Magnetics). Pharmacokinetics: S. Majumdar et al., Invest. Radiol. 25, 771 (1990). Physical and chemical properties: C. W. Jung, P. Jacobs, Magn. Reson. Imaging 13, 661 (1995). Surface properties: C. W. Jung, ibid. 675. Clinical studies in hepatic imaging: T. J. Vogl et al., Radiology 198, 881 (1996); E. Senéterre et al., ibid. 200, 785 (1996). Series of articles on toxicology: Jpn. Pharmacol. Ther. 22, 57-141 (1994). Review of physicochemical characteristics and clinical applications: O. Clement et al., Top. Magn. Reson. Imaging 9, 167-182 (1998).

Ferumoxsil CAS Registry Number: 171544-35-7

Trademarks: GastroMARK (Mallinckrodt); Lumiren (Guerbet)
Literature References: Active ingredient of colloidal super paramagnetic iron oxide (SPIO) consisting of nonstoichiometric magnetite cores coated with siloxane (FeOx[C3H13N2SiO2]y); designed for use as negative MRI contrast agent. Prepn: M. S. Chagnon et al., EP 125995, R. A. Whitehead et al., US 4554088 (1984, 1985 both to Advanced Magnetics). Physical and chemical properties: C. W. Jung, P. Jacobs, Magn. Reson. Imaging 13, 661 (1995). Surface properties: C. W. Jung, ibid. 675. Clinical study in lower abdominal imaging: R. C. H. Heusler et al., J. Magn. Reson. Imaging 4, 385 (1995); A. D'Arienzo et al., Am. J. Gastroenterol. 95, 720 (2000).

Dimethadione CAS Registry Number: 695-53-4 二甲双酮

CAS Name: 5,5-Dimethyl-2,4-oxazolidinedione
Additional Names: DMOTrademarks: Eupractone (Baxter)
Percent Composition: C 46.51%, H 5.46%, N 10.85%, O 37.18%
Literature References: Active metabolite of trimethadione, q.v. Prepn: F. Urech, Ber. 13, 485 (1880); R. W. Stoughton, J. Am. Chem. Soc. 63, 2376 (1941). Anticonvulsant activity: C. D. Withrow et al., J. Pharmacol. Exp. Ther. 161, 335 (1968); in comparison with trimethadione: H. Ferngren, Acta Pharmacol. Toxicol. 26, 177 (1968). Use in measurement of intracellular pH and cellular pH gradients: S. Addanki et al., J. Biol. Chem. 243, 2337 (1968); V. Ehrhardt, Biochim. Biophys. Acta 775, 182 (1984); J. B. Arnold et al., J. Cereb. Blood Flow Metab. 5, 369 (1985). GLC determn: W. Gazdzik, W. Kmiotek, J. Chromatogr. 378, 482 (1986); LC determn in serum: E. Tanaka, S. Misawa, J. Chromatogr. 413, 376 (1987).

Cynarin(e) CAS Registry Number: 30964-13-7 1,5-二咖啡酰奎宁酸; 洋蓟素

CAS Name: [1R-(1a,3a,4a,5b)]-1,3-Bis[[3-(3,4-dihydroxyphenyl)-1-oxo-2-propenyl]oxy]-4,5-dihydroxycyclohexanecarboxylic acid
Additional Names: 1,3-dicaffeoylquinic acid; 1,5-dicaffeylquinic acid...
Literature References: Active principle of artichoke, Cynara scolymus L., Compositae: L. Panizzi, M. L. Scarpati, Gazz. Chim. Ital. 84, 792 (1954). Synthesis of originally proposed structure: L. Panizzi et al., ibid. 806; L. Panizzi et al., US 2863909; US 3100224 (1958, 1963 both to Farmitalia); Alberti et al., US 2918477 (1959). Revised structure: L. Panizzi, M. L. Scarpati, Gazz. Chim. Ital. 95, 71 (1965). NMR confirmation of structure: I. Horman et al., J. Agric. Food Chem. 32, 538 (1984). HPLC determn in pharmaceutics: A. Bettero, Boll. Chim. Farm. 120, 49 (1981). Inhibition of fatty acid mobilization: P. Dorigo, G. Fassina, Pharmacol. Res. Commun. 2, 109 (1970). Reduction of cholesterol levels in rats: J. Wojcicki, Drug Alcohol Depend. 3, 143 (1978). Clinical trial in hyperlipemic syndrome: M. Montini et al., Arzneim.-Forsch. 25, 1311 (1975).

Asiaticoside CAS Registry Number: 16830-15-2 积雪草苷

CAS Name: (2a,3b,4a)-2,3,23-Trihydroxyurs-12-en-28-oic acid O-6-deoxy-a-L-mannopyranosyl-(1®4)-O-b-D-glucopyranosyl-(1®6)-O-b-D-glucopyranosyl ester
Percent Composition: C 60.11%, H 8.20%, O 31...
Literature References: Active principle of Centella asiatica (L.) Urban, Umbelliferae. Trisaccharide moiety linked to the aglycone: asiatic acid. Isoln: J.-E. Bontems, Bull. Sci. Pharmacol. 49, 186 (1941), C.A. 38, 4094 (1944); idem, Gaz. Med. Madagascar 5, 29 (1942). Structure of asiatic acid: J. Polonsky, Bull. Soc. Chim. Fr. 1953, 173. Structure of asiaticoside: P. Boiteau et al., Nature 163, 258 (1949); J. Polonsky et al., Bull. Soc. Chim. Fr. 1959, 880. Metabolism: L. F. Chasseaud et al., Arzneim.-Forsch. 21, 1379 (1971). Wound healing properties: H. Rosen et al., Proc. Soc. Exp. Biol. Med. 125, 279 (1967). Clinical study: J.-P. Bosse et al., Ann. Plast. Surg. 3, 13 (1979). Review on asiatic acid: J. L. Simonsen, W. C. J. Ross, The Terpenes vol. 5 (University Press, Cambridge, 1957) pp 58-67.

Aspidin CAS Registry Number: 584-28-1 绵马毒素BB

CAS Name: 2-[[2,6-Dihydroxy-4-methoxy-3-methyl-5-(1-oxobutyl)phenyl]methyl]-3,5-dihydroxy-4,4-dimethyl-6-(1-oxobutyl)-2,5-cyclohexadien-1-one
Additional Names: 3'-[(5-butyryl-2,4-dihydroxy-3,3-...
Literature References: Active principle of fern root: Boehm, Ann. 302, 171 (1898); 329, 321 (1903); from Dryopteris austriaca (Jacq.) Woynar, Polypodiaceae: Aebi et al., Helv. Chim. Acta 40, 266 (1957). Structure: eidem, ibid. 569. Synthesis: Riedl, Mitteldorf, Ber. 89, 2595 (1956).

Progesterone CAS Registry Number: 57-83-0 孕酮; 黄体素; 黄体酮

CAS Name: Pregn-4-ene-3,20-dione
Additional Names: D4-pregnene-3,20-dione; corpus luteum hormone; luteohormone
Trademarks: Crinone (Serono); Cyclogest (Alpharma); Estima (EFFIK); Gestone (No...
Literature References: Active principle of the corpus luteum, secreted during the latter half of the menstrual cycle. If pregnancy ensues, secretion continues. Exerts an antiovulatory effect when administered during days 5 to 25 of the normal menstrual cycle. Isoln from corpus luteum of pregnant sows: Butenandt, Westphal, Ber. 67, 1440 (1934); Wintersteiner, Allen, J. Biol. Chem. 107, 321 (1934). Structure: Butenandt et al., Ber. 67, 1611 (1934). Synthesis of DL-form: Johnson et al., J. Am. Chem. Soc. 93, 4332 (1971). Prepn from other steroids in review by W. H. Strain in Gilman's Organic Chemistry vol. II (Wiley, New York, 2nd ed., 1943) pp 1487-1489. Numerous patents, e.g., US 2379832; US 2232438; US 2314185. Anesthetic effect and toxicity: H. Selye, Proc. Soc. Exp. Biol. Med. 46, 116 (1941). Review of physiology: Csapo, Sci. Am. 198, 40-46 (April, 1958); Rothchild, Vitam. Horm. 23, 209-327 (1965). Book: Progesterone and Progestins, C. W. Bardin et al., Eds. (Raven Press, New York, 1982) 462 pp.

Picaridin CAS Registry Number: 119515-38-7 埃卡瑞丁

CAS Name: 2-(2-Hydroxyethyl)-1-piperidinecarboxylic acid 1-methylpropyl ester
Additional Names: icaridin; 1-methylpropyl 2-(2-hydroxyethyl)piperidine-1-carboxylate; hydroxyethyl isobutyl piperi...
Literature References: Acts on certain olfactory receptor cell types to reduce the activating or attracting effect of odor sources. Prepn: B.-W. Krüger et al., EP 289842; eidem, US 4900834 (1988, 1990 both to Bayer). Synthesis and mode of action: J. Boeckh et al., Pestic. Sci. 48, 359 (1996). Field trials in mosquito repellency: H. H. Yap et al., J. Vector Ecol. 23, 62 (1998); A. Badolo et al., Trop. Med. Int. Health 9, 330 (2004). Physical, chemical and toxicological properties: WHO Interim Specification for Icaridin (WHO/IS/TC/668/2001) 16 pp. MS characterization: T. P. Knepper, J. Chromatogr. A 1046, 159 (2004).

Strontium Lactate CAS Registry Number: 29870-99-3 乳酸锶(三水)

CAS Name: 2-Hydroxypropanoic acid strontium salt
Percent Composition: C 27.12%, H 3.79%, O 36.12%, Sr 32.97%
Literature References: Acute toxicity: K. W. Cochran et al., Arch. Ind. Hyg. Occup. Med. 1, 637 (1950).