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

Lupeol CAS Registry Number: 545-47-1 羽扇豆醇

CAS Name: (3b)-Lup-20(29)-en-3-ol
Additional Names: monogynol B; b-viscol; fagarasterol
Percent Composition: C 84.44%, H 11.81%, O 3.75%
Literature References: Abundant plant triterpene. Occurs in the skin of lupin seeds, in chicle, in the latex of fig trees and of rubber plants. Was detected in cocoons of Bombyx mori. Isoln: Cohen, Rec. Trav. Chim. 28, 368 (1909); Ruzicka et al., Helv. Chim. Acta 20, 1567 (1937). Identity with b-viscol: Meyer, Jeger, ibid. 31, 1868 (1948). Identity with monogynol B: Chatterji et al., J. Sci. Ind. Res. 18B, 262 (1959). Structure: Ruzicka et al., Helv. Chim. Acta 28, 942 (1945); Ames et al., J. Chem. Soc. 1951, 450. Structure of hydrochloride: Halsall et al., ibid. 1952, 2862. Configuration: Barton, Holmes, ibid. 1952, 78; Djerassi et al., J. Am. Chem. Soc. 77, 5330 (1955). NMR studies: Buckley et al., Chem. Ind. (London) 1971, 298. Total synthesis: Stork et al., J. Am. Chem. Soc. 93, 4945 (1971).

Norgestimate CAS Registry Number: 35189-28-7 炔诺肟酯

CAS Name: (17a)-17-(Acetyloxy)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one 3-oxime
Additional Names: (+)-13-ethyl-17-hydroxy-18,19-dinor-17a-pregn-4-en-20-yn-3-one oxime acetate (ester); 17a-ace...
Literature References: Acetate oxime of D-norgestrel, q.v. Prepn: A. P. Shroff, DE 2633210; idem, US 4027019 (both 1977 to Ortho). HPLC determn: P. A. Lane et al., J. Pharm. Sci. 76, 44 (1987). Pharmacology: D. W. Hahn et al., Contraception 16, 541 (1977); J. Killinger et al., ibid. 32, 311 (1985). Pharmacodynamics: H. S. Weintraub et al., J. Pharm. Sci. 67, 1406 (1978). Metabolism in female monkeys: S. F. Sisenwine et al., Contraception 15, 25 (1977); in women: K. B. Alton et al., ibid. 29, 19 (1984). Clinical trial as a contraceptive in combination with ethinyl estradiol: B. Rubio-Lotvin, R. Gonzales-Ansorena, Acta Eur. Fertil. 9, 1 (1978).

Imazamox CAS Registry Number: 114311-32-9 甲氧咪草烟

CAS Name: 2-[4,5-Dihydro-4-methyl-4-(1-methylethyl)-5-oxo-1H-imidazol-2-yl]-5-(methoxymethyl)-3-pyridinedicarboxylic acid
Additional Names: 2-(4-isopropyl)-4-methyl-5-oxo-2-imidazolin-2-yl-5-(m...
Literature References: Acetohydroxyacid synthase (AHAS) inhibitor. Prepn: R. F. Doehner, Jr., EP 254951; idem et al., US 5334576 (1988, 1994 both to Am. Cyanamid). Chemical and physical properties: G. R. Glover, Proc. South. Weed Sci. Soc. 48, 269 (1995). Metabolism study: B. Tecle et al., Brighton Crop Prot. Conf. - Weeds 1997, 605. CE determn in beans: K. Ohba et al., J. Pestic. Sci. 22, 277 (1997). Field trials: K. A. Nelson, K. A. Renner, Weed Technol. 12, 137 (1998); R. E. Blackshaw, ibid. 64. Soil persistence: T. Cobucci et al., Weed Sci. 46, 258 (1998). Review: T. M. Brady et al., ACS Symp. Ser. 686, 30-37 (1998).

Flucarbazone CAS Registry Number: 145026-88-6

CAS Name: 4,5-Dihydro-3-methoxy-4-methyl-5-oxo-N-[[2-(trifluoromethoxy)phenyl]sulfonyl]-1H-1,2,4-triazole-1-carboxamide
Percent Composition: C 36.37%, H 2.80%, F 14.38%, N 14.14%, O 24.22%, S 8...
Literature References: Acetolactate synthase inhibitor for control of weeds in wheat. Prepn: K.-H. Müller et al., EP 507171; eidem, US 5534486 (1992, 1996 both to Bayer). Comprehensive description: H. J. Santel et al., Brighton Crop Prot. Conf. - Weeds 1999, 23-28. Field trials in wheat: K. J. Kirkland et al., Weed Technol. 15, 48 (2001).

Imazosulfuron CAS Registry Number: 122548-33-8 咪唑磺隆

CAS Name: 2-Chloro-N-[[(4,6-dimethoxy-2-pyrimidinyl)amino]carbonyl]imidazo[1,2-a]pyridine-3-sulfonamide
Additional Names: 1-(2-chloroimidazo[1,2-a]pyridin-3-ylsulfonyl)-3-(4,6-dimethoxypyrimidi...
Literature References: Acetolactate-synthase (ALS) inhibitor; sulfonylurea herbicide for weed control in rice crops. Prepn: Y. Ishida et al., EP 238070; eidem, US 5017212 (1987, 1991 both to Takeda); eidem, J. Pestic. Sci. 18, 175 (1993). Mechanism of action study: Y. Tanaka, H. Yoshikawa, J. Weed Sci. Technol. 43, 291 (1998). Soil degradation studies: K. Mikata et al., J. Pestic. Sci. 26, 376 (2001). LC determn in water and soil: M. Ventriglia et al., J. Chromatogr. A 857, 327 (1999); in rice: Y. Akiyama et al., J. Food Hyg. Soc. Jpn. 43, 99 (2002). Review of development: H. Nagase, Agrochem. Jpn. 64, 15-16 (1994); and biological activity: Y. Ishida et al., J. Pestic. Sci. 21, 247-258 (1996).

Acetyltannic Acid CAS Registry Number: 1397-74-6 乙酰基鞣酸

Additional Names: Diacetyltannic acid; tannyl acetate
Trademarks: Acetannin; Tannigen
Literature References: Acetylation of tannin: Ciusa, Sollazzo, Ann. Chim. Appl. 33, 72 (1942); C.A. 38, 57944 (1944).

Physostigmine CAS Registry Number: 57-47-6 毒扁豆碱

CAS Name: (3aS-cis)-1,2,3,3a,8,8a-Hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-ol methylcarbamate (ester)
Additional Names: eserine
Trademarks: Synapton (Forest)
Percent Composition: C...
Literature References: Acetylcholinesterase inhibitor. From Calabar beans, the seeds of the vine Physostigma venenosum Balf., Leguminosae: Jobst, Hesse, Ann. 129, 115 (1864); Hesse, ibid. 141, 82 (1867). Extraction procedure: Schwyzer, Die Fabrikation pharmazeutischer und chemisch-technischer Produkte (Berlin, 1931) p 338; Chemnitius, J. Prakt. Chem. 116, 59 (1927). Structure: Stedman, Barger, J. Chem. Soc. 127, 247 (1925). Absolute configuration: R. B. Longmore, B. Robinson, Chem. Ind. (London) 1969, 622. Crystal structure: Petcher, Pauling, Nature 241, 277 (1973). Synthesis: Julian, Pikl, J. Am. Chem. Soc. 57, 755 (1935); Harley-Mason, Jackson, J. Chem. Soc. 1954, 3651; J. Wijnberg, W. N. Speckamp, Tetrahedron 34, 2399 (1978). Cholinesterase inhibitor: Engelhart, Loewi, Arch. Exp. Pathol. Pharmakol. 150, 1 (1930); Matthes, J. Physiol. 70, 338 (1930). Toxicity data: W. T. Lynch, J. M. Coon, Toxicol. Appl. Pharmacol. 21, 53 (1972); R D. Sofia, L. C. Knabloch, ibid. 28, 227 (1974). Improvement of long-term memory: K. L. Davis et al., Science 201, 272 (1978). Memory enhancement in Alzheimer's disease: L. J. Thal et al., N. Engl. J. Med. 308, 720 (1983); eidem, Ann. Neurol. 13, 491 (1983); L. Gustafson et al., Psychopharmacology 93, 31 (1987). Review: B. Robinson in The Alkaloids Vol. XIII, R. H. F. Manske, Ed. (Academic Press, New York, 1971) pp 213-226. Comprehensive description: F. J. Muhtadi, S. S. El-Hawary, Anal. Profiles Drug Subs. 18, 289-350 (1989).

Donepezil CAS Registry Number: 120014-06-4 多萘哌齐碱

CAS Name: 2,3-Dihydro-5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-1H-inden-1-one
Additional Names: 5,6-dimethoxy-2-[[1-(phenylmethyl)-4-piperidinyl]methyl]-2,3-dihydro-1H-inden-1-o...
Literature References: Acetylcholinesterase inhibitor. Prepn: H. Sugimoto et al., EP 296560, eidem, US 4895841 (1988, 1990 both to Eisai). Synthesis: Y. Iimura et al., J. Labelled Compd. Radiopharm. 27, 835 (1989). Resolution of enantiomers: J. Haginaka, C. Seyama, J. Chromatogr. B 577, 95 (1992). Clinical pharmacokinetics: A. Ohnishi et al., J. Clin. Pharmacol. 33, 1086 (1993). Clinical trials in Alzheimer's disease: R. C. Mohs et al., Neurology 57, 481 (2001); B. Winblad et al., ibid. 489. Review of pharmacology and clinical experience in cognitive disorders: G. C. Román, S. J. Rogers, Expert Opin. Pharmacother. 5, 161-180 (2004).

Tazarotene CAS Registry Number: 118292-40-3 他扎罗汀

CAS Name: 6-[(3,4-Dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)ethynyl]-3-pyridinecarboxylic acid ethyl ester
Additional Names: ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl] nicotinateTrad...
Literature References: Acetylenic retinoid prodrug converted to the active metabolite, tazarotenic acid, with selective affinity for retinoic acid receptors RARb and RARg. Prepn: R. A. S. Chandraratna, EP 284288; idem, US 5089509 (1988, 1992 both to Allergan). Clinical evaluation in psoriasis: T. Esgleyes-Ribot et al., J. Am. Acad. Dermatol. 30, 581 (1994). Clinical trial in treatment of photodamage: S. Kang et al., ibid. 52, 268 (2005). Review of pharmacokinetics and metabolism: D. D.-S. Tang-Liu et al., Clin. Pharmacokinet. 37, 273-287 (1999); of mechanism of action and treatment strategies: A. Roeder et al., Skin Pharmacol. Physiol. 17, 111-118 (2004).

Mukaiyama Reagent CAS Registry Number: 14338-32-0 2-氯-1-甲基吡啶碘化物

CAS Name: 2-Chloro-1-methylpyridinium iodide
Additional Names: 2-chloropyridine methiodide; 1-methyl-2-chloropyridinium iodide
Percent Composition: C 28.21%, H 2.76%, Cl 13.88%, I 49.67%, N ...
Literature References: Acid-activating agent for prepn of carboxylic esters. Prepn: M. Liveris, J. Miller, Aust. J. Chem. 2, 297 (1958); and reactions with hydroxide ions: G. B. Barlin, J. A. Benbow, J. Chem. Soc. Perkin Trans. 2 1974, 790. Use in synthesis of carboxylic esters: T. Mukaiyama et al., Chem. Lett. 1975, 1045; T. Mukaiyama, Angew. Chem. Int. Ed. 18, 707 (1979). Kinetic resolution of carboxylic acids and alcohols: A. Mazón et al., Tetrahedron: Asymmetry 3, 1455 (1992). Kinetics of nucleophilic substitution reactions with primary and secondary amines: A. Awwal et al., Indian J. Chem. 40B, 32 (2001); with phenols: M. Kabir et al., ibid. 43B, 1779 (2004). Use in synthesis of ketenes: R. L. Funk et al., Synlett 1989, 36; of b-lactams: C. M. L. Delpiccolo et al., J. Comb. Chem. 5, 208 (2003); of esters: D. Donati et al., Tetrahedron Lett. 46, 2817 (2005).