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

Sematilide CAS Registry Number: 101526-83-4 司美利特盐酸盐

CAS Name: N-[2-(Diethylamino)ethyl]-4-[(methylsulfonyl)amino]benzamidePercent Composition: C 53.65%, H 7.40%, N 13.41%, O 15.31%, S 10.23%
Literature References: Prepn: D. D. Davey et al., US 4544654 (1985 to Schering AG); W. C. Lumma, Jr. et al., J. Med. Chem. 30, 755 (1987). Pharmacology: S. S. Greenberg et al., Drug Dev. Res. 25, 283 (1992). Pharmacokinetics and HPLC determn in plasma: S. Dancik et al., J. Pharm. Sci. 80, 157 (1991). Clinical pharmacology: W. Wong et al., Am. J. Cardiol. 69, 206 (1992). Electrophysiologic profile: P. T. Sager et al., Circulation 88, 1072 (1993). Review: T. A. Argentieri, Cardiovasc. Drug Rev. 10, 182-198 (1992).

Benoxaprofen CAS Registry Number: 67434-14-4 苯噁洛芬

CAS Name: 2-(4-Chlorophenyl)-a-methyl-5-benzoxazoleacetic acidTrademarks: Coxigon (Lilly); Opren (Lilly); Oraflex (Lilly)
Percent Composition: C 63.69%, H 4.01%, Cl 11.75%, N 4.64%, O 15.91%
Literature References: Prepn: D. Evans et al., DE 2324443; eidem, US 3912748 (1973, 1975 both to Lilly); D. W. Dunwell et al., J. Med. Chem. 18, 53 (1975). Analysis by HPLC: S. W. McKay et al., J. Chromatogr. 170, 482 (1979). Pharmacokinetics: D. H. Chatfield et al., Br. J. Clin. Pharmacol. 4, 579 (1977). Metabolism: D. H. Chatfield, J. N. Green, Xenobiotica 8, 133 (1978). Effect on lysosomal enzyme secretion: R. J. Smith, J. Pharmacol. Exp. Ther. 207, 618 (1978). Dissolution and absorption in humans: A. S. Ridolfo et al., J. Pharm. Sci. 68, 850 (1979). Series of clinical studies: Rheumatol. Rehabil. 17, 254-264 (1978). Retrospective study of molecular toxicology: D. F. V. Lewis et al., Toxicology 65, 33 (1990).

Trimethyl Isopropyl Butanamide CAS Registry Number: 51115-67-4 N,2,3-三甲基-2-异丙基丁酰胺

CAS Name: N,2,3-Trimethyl-2-(1-methylethyl)butanamide
Additional Names: 2-isopropyl-N,2,3-dimethylbutanamidePercent Composition: C 70.12%, H 12.36%, N 8.18%, O 9.34%
Literature References: Prepn: D. G. Rowsell et al., DE 2317538; eidem, US 4296255 (1973, 1981 both to Wilkinson Sword). Structure-activity study: H. R. Watson et al., J. Soc. Cosmet. Chem. 29, 185 (1978). Brief review: M. A. Parrish, Manuf. Chem. 58, 31-32 (February, 1987).

Clemizole CAS Registry Number: 442-52-4 克立咪唑

CAS Name: 1-[(4-Chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole
Additional Names: 1-(p-chlorobenzyl)-2-(1-pyrrolidinylmethyl)benzimidazole; 1-(p-chlorobenzyl)-2-pyrrolidylmethyle...
Literature References: Prepn: D. Jerchel et al., Ann. 575, 162 (1952); GB 703272; M. Schenck, W. Heinz, US 2689853 (both 1954 to Schering A.G.).

Protionamide CAS Registry Number: 14222-60-7 丙硫异烟胺

CAS Name: 2-Propyl-4-pyridinecarbothioamide
Additional Names: 2-propylthioisonicotinamide; prothionamide; 2-propyl-4-thiocarbamoylpyridine
Trademarks: Ektebin (Hefa); Peteha (Fatol); Trevint...
Literature References: Prepn: D. Liberman et al., Compt. Rend. 242, 2409 (1956); GB 800250, D. Liberman, US 2901488 (1958, 1959 both to Chimie et Atomistique); L. N. Yakhontov et al., Khim. Farm. Zh. 10, 96 (1976), C.A. 85, 32787h (1976). Pharmacology: A. M. Il'in, Farmakol. Toksikol. 38, 471 (1975).

Octenidine CAS Registry Number: 71251-02-0 奥克太啶

CAS Name: N,N'-(1,10-Decanediyldi-1(4H)-pyridinyl-4-ylidene)bis[1-octanamine]
Additional Names: 1,10-bis-[4-(octylamino)-1-pyridinium]decanePercent Composition: C 78.49%, H 11.34%, N 10.17%
Literature References: Prepn: D. M. Bailey, BE 851807; idem, US 4206215 (1977, 1980 both to Sterling); D. M. Bailey et al., J. Med. Chem. 27, 1457 (1984). Structure-activity study: A. M. Slee et al., Antimicrob. Agents Chemother. 23, 531 (1983). Antiplaque activity: A. M. Slee, J. R. O'Connor, ibid. 379; microbiocidal activity: D. M. Sedlock, D. M. Bailey, ibid. 28, 786 (1985). Antimycotic effects: M. A. Ghannoum et al., J. Antimicrob. Chemother. 25, 237 (1990). Clinical evaluation as topical disinfectant: B. Christiansen, Z. Bakteriol. Mikrobiol. Hyg. 186, 368 (1988). Clinical trials in prevention of plaque and gingivitis: M. R. Patters et al., J. Periodontal Res. 21, 154 (1986); B. B. Beiswanger et al., J. Dent. Res. 69, 454 (1990).

Quinfamide CAS Registry Number: 62265-68-3 1-(二氯乙酰基)-6-(2-呋喃甲酰氧基)-1,2,3,4-四氢喹啉

CAS Name: 2-Furancarboxylic acid 1-(dichloroacetyl)-1,2,3,4-tetrahydro-6-quinolinyl ester
Additional Names: 2-furoic acid ester with 1-(dichloroacetyl)-1,2,3,4-tetrahydro-6-quinolinol; 1-(dichl...
Literature References: Prepn: D. M. Bailey, US 3997542 (1976 to Sterling); D. M. Bailey et al., J. Med. Chem. 22, 600 (1979). Amebicidal activity and toxicological evaluation: R. G. Slighter et al., Parasitology 81, 157 (1980). Distribution and metabolism in rats: J. F. Baker, Arch. Int. Pharmacodyn. 258, 29 (1982). HPLC determn in biological samples: J. M. Morales et al., J. Chromatogr. B 746, 133 (2000). Clinical evaluation in adults with chronic amebiasis: L. Guevara et al., Clin. Ther. 6, 43 (1983); in children: F. A. Rojas et al., ibid. 47.

Vinclozolin CAS Registry Number: 50471-44-8 乙烯菌核利

CAS Name: 3-(3,5-Dichlorophenyl)-5-ethenyl-5-methyl-2,4-oxazolidinedione
Additional Names: 3-(3,5-dichlorophenyl)-5-methyl-5-vinyloxazolidine-2,4-dioneTrademarks: Ronilan (BASF); Vorlan (Mallin...
Literature References: Prepn: D. Mangold et al., DE 2207576 (1973 to BASF), C.A. 79, 137120q (1973). Activity: C. Hess, F. Locher, Proc. Brit. Insectic. Fungic. Conf. 2, 693 (1975). Comparative mechanism of action: A. C. Pappas, D. J. Fisher, Pestic. Sci. 10, 239 (1979).

Oxazidione CAS Registry Number: 27591-42-0 奥沙二酮

CAS Name: 2-(4-Morpholinylmethyl)-2-phenyl-1H-indene-1,3(2H)-dione
Additional Names: 2-phenyl-2-morpholinomethylindane-1,3-dione; mofedioneTrademarks: Transidione (Dausse); Amplidione (Dausse)<...
Literature References: Prepn: D. P. R. Giudicelli, H. Najer, ZA 69 02814 (1969 to Lab. Dausse), C.A. 72, 111159q (1970).

Diethylmalonic Acid CAS Registry Number: 510-20-3 二乙基丙二酸

CAS Name: Diethylpropanedioic acid
Additional Names: 3,3-pentanedicarboxylic acid
Percent Composition: C 52.49%, H 7.55%, O 39.96%
Literature References: Prepn: Daimler, Ann. 249, 173 (1888); Speck, J. Am. Chem. Soc. 74, 2876 (1952). Spectral studies: J. L. Delarbre et al., J. Raman Spectrosc. 16, 11 (1985). Crystal structure: A. Dubourg et al., Acta Crystallogr. C44, 1987 (1988).