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

Sucralose CAS Registry Number: 56038-13-2 三氯蔗糖

CAS Name: 1,6-Dichloro-1,6-dideoxy-b-D-fructofuranosyl-4-chloro-4-deoxy-a-D-galactopyranoside
Additional Names: 4,1',6'-trichloro-4,1',6'-trideoxy-galacto-sucrose; 1',4,6'-trichlorogalactosucro...
Literature References: Chlorinated sucrose derivative with enhanced sweetness. Prepn: P. H. Fairclough et al., Carbohydr. Res. 40, 285 (1975). Prepn of crystalline anhydrous and pentahydrate: M. R. Jenner, D. Waite, EP 30804 (1981 to Tate Lyle; Talres Dev.); eidem, US 4343934 (1982 to Talres Dev.). Use as non-nutritive sweetener: BE 850180; L. Hough et al., US 4435440 (1977, 1984 both to Tate Lyle). In vitro activity vs cariogenic bacteria: J. Verran, D. B. Drucker, Arch. Oral Biol. 27, 693 (1982). Structure-sweetness relationship: M. Mathlouthi et al., Carbohydr. Res. 152, 47 (1986). Review: L. Hough, R. Khan, Trends Biochem. Sci. 3, 61-63 (1978).

Erdin CAS Registry Number: 26891-81-6 螺内酯[苯并呋喃-2(3H),1'-[2,5]环己二烯]-2'-羧酸,5,7-二氯-4-羟基-6'-甲氧基-6-甲基-3,4'-二氧基-

CAS Name: 5,7-Dichloro-4-hydroxy-6'-methoxy-6-methyl-3,4'-dioxospiro[benzofuran-2(3H),1'-[2,5]cyclohexadiene]-2'-carboxylic acid
Additional Names: dl-erdin
Percent Composition: C 49.90%, H 2...
Literature References: Chlorine containing fungal metabolite isolated from Aspergillus terreus Thom, as the racemate, together with geodin: H. Raistrick, G. Smith, Biochem. J. 30, 1315 (1936). Characterization and structure of erdin and geodin: P. W. Clutterbuck et al., ibid. 31, 1089 (1937); C. T. Calam et al., ibid. 33, 579 (1939); eidem, ibid. 41, 458 (1947); D. H. Barton, A. I. Scott, J. Chem. Soc. 1958, 1767. Biosynthesis of geodin: Rhodes et al., Chem. Ind. (London) 1962, 611.

Chlorobutanol CAS Registry Number: 57-15-8 三氯叔丁醇

CAS Name: 1,1,1-Trichloro-2-methyl-2-propanol
Additional Names: b,b,b-trichloro-tert-butyl alcohol; acetone chloroform; chlorbutol
Trademarks: Chloretone (Parke-Davis); Coliquifilm (Allergan...
Literature References: Chlorobutanol may be anhydrous or it may contain up to about one-half molecule of water. Prepn: Fishburn, Watson, J. Am. Pharm. Assoc. 28, 491 (1939); E. Bergman, US 2446453 (1948 to Polymerisable Products Ltd.); P. Riegger, H. Richtzenbain, DE 1271697 (1968 to Dynamit Nobel A.-G.), C.A. 69, 95967g (1968); M. Saljoughian, Monatsh. Chem. 114, 813 (1983). Toxicity studies: E. Impens, Arch. Int. Pharmacodyn. Ther. 8, 77 (1901).

Nimustine CAS Registry Number: 42471-28-3 尼莫司汀

CAS Name: N'-[(4-Amino-2-methyl-5-pyrimidinyl)methyl]-N-(2-chloroethyl)-N-nitrosourea
Percent Composition: C 39.64%, H 4.81%, Cl 13.00%, N 30.82%, O 11.73%
Literature References: Chloroethylnitrosourea derivative with antitumor activity. Prepn: H. Nakao et al., DE 2257360; eidem, US 4003901 (1973, 1977 both to Sankyo); eidem, Yakugaku Zasshi 94, 1932 (1974), C.A. 82, 43263y (1975). Effects on macrophage cytostatic activity in rats: N. Saijo et al., Br. J. Cancer 42, 162 (1980). Distribution, excretion, metabolism in mice: M. Tanaka et al., Cancer Treat. Rep. 64, 575 (1980). Exptl and clinical effect: N. Saijo et al., Cancer Chemother. Pharmacol. 4, 165 (1980). Acute toxicity: H. Masuda et al., Sankyo Kenkyusho Nempo 29, 118 (1977), C.A. 88, 146298s (1978).

Ranimustine CAS Registry Number: 58994-96-0 雷莫司汀

CAS Name: Methyl 6-[[[(2-chloroethyl)nitrosoamino]carbonyl]amino]-6-deoxy-a-D-glucopyranoside
Additional Names: methyl N-carbamyl-N'-(2-chloroethyl)-N'-nitroso-6-amino-6-deoxy-a-D-glucopyranosi...
Literature References: Chloroethylnitrosourea derivative with antitumor activity. Similar to carmustine, chlorozotocin, lomustine, nimustine, q.q.v. Prepn: NL 7507973; G. Kimura, J. Sekine, US 4057684; NL 7800920; G. Kimura, US 4156777 (1976, 1977, 1978, 1979, all to Tokyo Tanabe). Antitumor activity in rodents, comparison with other nitrosoureas: S. Sekido et al., Cancer Treat. Rep. 63, 961 (1979); S. Fujimoto, M. Ogawa, Cancer Chemother. Pharmacol. 9, 134 (1982); S. Fujimoto et al., Gann 75, 937 (1984). Mechanism of action: R. Kanamaru et al., Curr. Chemother. Immunother. 2, 1377 (1982). Effect of sugar alcohols on toxicity in mice: T. Tashiro et al., Cancer Chemother. Pharmacol. 8, 183 (1982). Series of articles on metabolic fate in rats: Y. Esumi et al., Iyakuhin Kenkyu 16, 381-428 (1985), C.A. 103, 115620q, 115621r, 134369f (1985). Clinical study in hematological malignant diseases: T. Masaoka et al., Chemotherapy (Tokyo) 33, 271 (1985).

Lomustine CAS Registry Number: 13010-47-4 洛莫司汀

CAS Name: N-(2-Chloroethyl)-N'-cyclohexyl-N-nitrosourea
Additional Names: 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosoureaTrademarks: Belustine (Bellon); CCNU (Lundbeck); Cecenu (Medac); CeeNU (BMS...
Literature References: Chloroethylnitrosourea derivative with antitumor activity. Similar to carmustine, chlorozotocin, nimustine, ranimustine, q.q.v. Synthesis: T. P. Johnston et al., J. Med. Chem. 9, 892 (1966). Clinical review: S. K. Carter, J. W. Newman, Cancer Chemother. Rep. Part 3 1, 136 (1968). Physiological disposition: V. T. Oliverio et al., Cancer Res. 30, 1330 (1970). Toxicology and pharmacology: G. R. Thompson, R. E. Larson, Toxicol. Appl. Pharmacol. 21, 405 (1972); V. T. Oliverio, Cancer Chemother. Rep. Part 3 4, 13 (1973). Comprehensive description: F. J. Al-Shammary, Anal. Profiles Drug Subs. 19, 315-340 (1990).

Chlorozotocin CAS Registry Number: 54749-90-5 氯脲霉素

CAS Name: 2-[[[(2-Chloroethyl)nitrosoamino]carbonyl]amino]-2-deoxy-D-glucose
Additional Names: 2-[3-(2-chloroethyl)-3-nitrosoureido]-2-deoxy-D-glucopyranose; 1-(2-chloroethyl)-1-nitroso-3-(D-gl...
Literature References: Chloroethylnitrosourea derivative with antitumor activity. Similar to carmustine, lomustine, nimustine, ranimustine, q.q.v; 2-chloroethyl analog of streptozotocin, q.v. Synthesis: H. D. Burns et al., Org. Prep. Proced. Int. 6, 259 (1974); T. P. Johnston et al., J. Med. Chem. 18, 104 (1975). Pharmacology: T. Anderson et al., Cancer Res. 35, 761 (1975); P. S. Schein et al., Cancer Treat. Rep. 60, 801 (1976). Decomposition in aqueous media: J. A. Montgomery et al., J. Med. Chem. 18, 568 (1975).

Carmustine CAS Registry Number: 154-93-8 卡莫司汀

CAS Name: N,N'-Bis(2-chloroethyl)-N-nitrosourea
Additional Names: BCNUTrademarks: Becenun (BMS); Bicnu (BMS); Carmubris (BMS)
Percent Composition: C 28.06%, H 4.24%, Cl 33.13%, N 19.63%, O 1...
Literature References: Chloroethylnitrosourea derivative with antitumor activity. Similar to chlorozotocin, lomustine, nimustine, ranimustine, q.q.v. Synthesis: Johnston et al., J. Med. Chem. 6, 669 (1963). Properties: Loo et al., J. Pharm. Sci. 55, 492 (1966). Decompn studies as related to antileukemic activity: Montgomery et al., J. Med. Chem. 10, 668 (1967). Antifungal action: Hunt, Pittilo, Antimicrob. Agents Chemother. 1965, 710. Toxicology studies: Thompson, Larson, Toxicol. Appl. Pharmacol. 21, 405 (1972). Review of pulmonary toxicity: A. C. Smith, Pharmacol. Ther. 41, 443-460 (1989).

Nitenpyram CAS Registry Number: 150824-47-8 烯啶虫胺

CAS Name: (1E)-N-[(6-Chloro-3-pyridinyl)methyl]-N-ethyl-N'-methyl-2-nitro-1,1-ethenediamine
Additional Names: 1-[N-(6-chloro-3-pyridylmethyl)-N-ethyl]amino-1-methylamino-2-nitroethyleneTrademar...
Literature References: Chloronicotinyl insecticide; orally administered flea adulticide. Prepn: I. Minamida et al., EP 302389; eidem, US 5849768 (1989, 1998 both to Takeda); and insecticidal activity: eidem, J. Pestic. Sci. 18, 41 (1993). Physical and biological properties: Y. Kashiwada, Agrochem. Jpn. 68, 18 (1996). Effects on neuronal nicotinic acetylcholine receptor channel in rat cells: K. Nagata et al., J. Pestic. Sci. 24, 143 (1999). Efficacy study in flea infested dogs: M.-C. Cadiergues et al., Am. J. Vet. Res. 60, 1122 (1999). LC-MS determn in fruits and vegetables: D. Zywitz et al., Deutsche Lebens.-Rundschau 99, 188 (2003).

Ezetimibe CAS Registry Number: 163222-33-1 依泽替米贝

CAS Name: (3R,4S)-1-(4-Fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)-2-azetidinoneTrademarks: Ezetrol (Merck/Schering-Plough); Zetia (Merck/Schering-Plough)
Perc...
Literature References: Cholesterol absorption inhibitor. Prepn: S. B. Rosenblum et al., WO 9508532; eidem, US 5767115 (1995, 1998 both to Schering); idem et al., J. Med. Chem. 41, 973 (1998). Enantioselective synthesis: G. Wu et al., J. Org. Chem. 64, 3714 (1999). Activity in animals: M. van Heek et al., J. Pharmacol. Exp. Ther. 283, 157 (1997). Metabolism and distribution: eidem, Br. J. Pharmacol. 129, 1748 (2000). Review of pharmacology and clinical studies: H. Bays, Expert Opin. Invest. Drugs 11, 1587-1604 (2002).