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

Primisulfuron-methyl CAS Registry Number: 86209-51-0 氟嘧磺隆

CAS Name: 2-[[[[[4,6-Bis(difluoromethoxy)-2-pyrimidinyl]amino]carbonyl]amino]sulfonyl]benzoic acid methyl ester
Additional Names: 2-[3-(4,6-bis(difluoromethoxy)pyrimidin-2-yl)ureidosulfonyl]ben...
Literature References: Post-emergence sulfonylurea herbicide. Prepn: W. Meyer et al., EP 84020; eidem, US 4478635 (1983, 1984 both to Ciba-Geigy). Comprehensive description: W. Maurer et al., Proc. Br. Crop Prot. Conf. - Weeds 1987, 41-48. Field trial in corn: C. L. Foy, H. L. Witt, Weed Technol. 4, 615 (1990).

Flumiclorac CAS Registry Number: 87547-04-4 氟烯草酸

CAS Name: [2-Chloro-4-fluoro-5-(1,3,4,5,6,7-hexahydro-1,3-dioxo-2H-isoindol-2-yl)phenoxy]acetic acid
Additional Names: 2-chloro-4-fluoro-5-[(3,4,5,6-tetrahydro)phthalimido]phenoxyacetic acid; [...
Literature References: Postemergent herbicide for use in food crops. Prepn: E. Nagano et al., EP 83055; eidem, US 4770695 (1983, 1988 both to Sumitomo). Comprehensive description: K. Kamoshita et al., in Pest Management in Soybean, L. G. Copping et al., Eds. (Elsevier, London, 1992) pp 317-324.

Fampridine CAS Registry Number: 504-24-5 4-氨基吡啶

CAS Name: 4-Pyridinamine
Additional Names: 4-aminopyridine; g-aminopyridine; 4-pyridylamine; 4-APPercent Composition: C 63.81%, H 6.43%, N 29.77%
Literature References: Potassium channel blocker. Prepn: A. Kirpal, Monatsh. Chem. 23, 244 (1902); R. Camps, Arch. Pharm. 240, 345 (1902); C. R. Hauser, G. A. Reynolds, J. Org. Chem. 15, 1224 (1950). Prolongs action potential in demyelinated nerve fibers: R. M. Sherratt et al., Nature 283, 570 (1980). HPLC determn in serum: A. van der Horst et al., J. Chromatogr. 574, 166 (1992). Neurophysiology and clinical efficacy in multiple sclerosis: H. A. M. van Diemen et al., J. Neurol. Sci. 116, 220 (1993). Clinical evaluation: C. H. Polman et al., Arch. Neurol. 51, 1136 (1994). Review of pharmacology and efficacy of aminopyridines in MS: C. T. Bever, Jr., Ann. Neurol. 36, S118-S121 (1994).

Dofetilide CAS Registry Number: 115256-11-6 多非利特

CAS Name: N-[4-[2-[Methyl[2-[4-[(methylsulfonyl)amino]phenoxy]ethyl]amino]ethyl]phenyl]methanesulfonamide
Additional Names: 1-(4-methanesulfonamidophenoxy)-2-[N-(4-methanesulfonamidophenethyl)-...
Literature References: Potassium channel blocker. Prepn: J. E. Arrowsmith et al., EP 245997; P. E. Cross et al., US 4959366 (1987, 1990 both to Pfizer); idem et al., J. Med. Chem. 33, 1151 (1990). HPLC determn in urine: D. K. Walker et al., J. Chromatogr. 568, 475 (1991). Mechanism of action study: D. Carmeliet, J. Pharmacol. Exp. Ther. 262, 809 (1992). Review of pharmacology and pharmacokinetics: H. S. Rasmussen et al., ibid. 20, Suppl. 2, S96-S105 (1992). Clinical trial in atrial fibrillation and flutter: B. L. Norgaard et al., Am. Heart J. 137, 1062 (1999); in congestive heart failure: C. Torp-Pedersen et al., N. Engl. J. Med. 341, 857 (1999).

Azimilide CAS Registry Number: 149908-53-2 阿齐利特

CAS Name: 1-[[[5-(4-Chlorophenyl)-2-furanyl]methylene]amino]-3-[4-(4-methyl-1-piperazinyl)butyl]-2,4-imidazolidinedione
Percent Composition: C 60.32%, H 6.16%, Cl 7.74%, N 15.29%, O 10.48%
Literature References: Potassium channel blocker. Prepn: S. S. Pelosi et al., WO 9304061 (1993 to Procter Gamble); C.-N. Yu et al., US 5462940 (1995 to Norwich Eaton). Clinical pharmacokinetics: A. Corey et al., J. Clin. Pharmacol. 37, 946 (1997). Clinical trial to improve post-infarct survival: A. J. Camm et al., Am. J. Cardiol. 81, Suppl. 6A, 35D (1998). Review of electrophysiologic properties and pharmacology: R. Karam et al., ibid. 40D-46D.

Tedisamil CAS Registry Number: 90961-53-8 替地沙米

CAS Name: 3',7'-Bis(cyclopropylmethyl)spiro[cyclopentane-1,9'-[3,7]diazabicyclo[3.3.1]nonane]
Percent Composition: C 79.11%, H 11.18%, N 9.71%
Literature References: Potassium channel blocking bradycardic agent. Prepn: U. Schön et al., DE 3234697; eidem, US 4550112 (1984, 1985 both to Kali-Chemie); and pharmacology: idem et al., J. Med. Chem. 41, 318 (1998). Suppression of the outward transient K+ current in rat myocytes: I. D. Dukes, M. Morad, Am. J. Physiol. 275, H1746 (1989). Toxicity in rats: E. Hayes et al., Pharmacol. Toxicol. 73, 257 (1993). Comparative clinical study in coronary artery disease: V. Mitrovic, et al., Clin. Cardiol. 21, 492 (1998). Clinical study in stable angina: K. M. Fox et al., Heart 83, 167 (2000). Review of pharmacology and clinical development: B. Freestone, G. Y. H. Lip, Expert Opin. Invest. Drugs 13, 151-160 (2004).

Levcromakalim CAS Registry Number: 94535-50-9 左色满卡林

CAS Name: (3S-trans)-3,4-Dihydro-3-hydroxy-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-2H-1-benzopyran-6-carbonitrile
Additional Names: (3S,4R)-3-hydroxy-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-6-chrom...
Literature References: Potassium channel opener. Prepn of racemate: J. M. Evans et al., EP 76075; eidem, US 4446113 (1983, 1984 both to Beecham); of isomers: E. Faruk, EP 120428 (1984 to Beecham); V. A. Ashwood et al., J. Med. Chem. 29, 2194 (1986). Mechanism of action and hemodynamic effects: R. P. Hof et al., Circ. Res. 62, 679 (1988). Pharmacology: J. C. Clapham et al., Arzneim.-Forsch. 41, 385 (1991). Clinical evaluation in hypertension: S. Suzuki et al., ibid. 45, 859 (1995).

Pinacidil CAS Registry Number: 60560-33-0 吡那地尔

CAS Name: N-Cyano-N'-4-pyridinyl-N''-(1,2,2-trimethylpropyl)guanidinePercent Composition: C 63.65%, H 7.81%, N 28.55%
Literature References: Potassium channel opening vasodilator. Prepn: H. J. Petersen, DE 2557438; idem, US 4057636 (1976, 1977 both to Leo Pharm.); H. J. Petersen et al., J. Med. Chem. 21, 773 (1978). Mechanism of action: E. Arrigoni-Martelli et al., Experientia 36, 445 (1980); K. M. Bray et al., Br. J. Pharmacol. 91, 421 (1987). Metabolism: E. Eilertsen et al., Xenobiotica 12, 187 (1982). Bioavailability: eidem, ibid. 177. Determn in plasma: M. Hamilton et al., J. Chromatogr. 375, 359 (1986). Pharmacokinetics and hypotensive effects: J. W. Ward et al., Eur. J. Clin. Pharmacol. 26, 603 (1984). Clinical comparison with hydralazine, q.v.: R. L. Byyny et al., Clin. Pharmacol. Ther. 42, 50 (1987). Review of pharmacology and mechanism of action: M. L. Cohen: Drug Dev. Res. 9, 249-258 (1986).

Myxin CAS Registry Number: 13925-12-7 堆囊粘菌素

CAS Name: 6-Methoxy-1-phenazinol 5,10-dioxide
Additional Names: 1-hydroxy-6-methoxyphenazine 5,10-dioxide; 3C antibiotic
Percent Composition: C 60.47%, H 3.90%, N 10.85%, O 24.78%
Literature References: Potent broad-spectrum antibiotic capable of inhibiting a wide range of gram-positive and gram-negative bacteria, various fungi and yeasts. Isoln from a Sorangium species (strain 3C), a soil-borne myxobacter: Peterson et al., Can. J. Microbiol. 12, 221 (1966). Proposed structure: Edwards, Gillespie, Tetrahedron Lett. 1966, 4867. Revised structure and synthesis: Weigele, Leimgruber, ibid. 1967, 715; Sigg, Toth, Helv. Chim. Acta 50, 716 (1967). Activity: E. Grunberg et al., Chemotherapia 12, 272 (1967). Crystal structure: Hanson, Acta Crystallogr. B24, 1084 (1968). Review: Edwards, Gillespie, Proc. Int. Symp. Drug Res. 1967, 236; Leimgruber, Grunberg, ibid. 240; Baker, Vezina, ibid. 242.

N-Ethyl-N-nitrosourea CAS Registry Number: 759-73-9 1-乙基-1-亚硝基脲

Additional Names: N-Nitroso-N-ethylurea; ENU
Percent Composition: C 30.77%, H 6.02%, N 35.88%, O 27.32%
Literature References: Potent mouse mutagen. Prepn: E. A. Werner, J. Chem. Soc. 115, 1093 (1919); F. Arndt, H. Scholz, Angew. Chem. 46, 47 (1933). Carcinogenicity studies: M. F. Rajewsky, R. Goth, Mol. Base Malig., Sel. Pap. Int. Symp. 1976, 2. Mutagenicity studies: W. L. Russell et al., Proc. Natl. Acad. Sci. USA 16, 5818 (1979). Toxicity studies: H. Druckrey et al., Nature 210, 1378 (1966).