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

Meralluride CAS Registry Number: 8069-64-5 美拉鲁利

CAS Name: [3-[[[(3-Carboxylato-1-oxopropyl)amino]carbonyl]amino]-2-methoxypropyl]hydroxymercurate(1-) sodium, mixture with 3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione
Additional Names: N-[[2-m...
Literature References: Structure: Pearson, Sigal, J. Org. Chem. 15, 1055 (1950). Toxicity data: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971).

N,N-Diethylphenylacetamide CAS Registry Number: 2431-96-1 N,N-二乙基苯乙酰胺

CAS Name: N,N-Diethylbenzeneacetamide
Additional Names: DEPA
Percent Composition: C 75.35%, H 8.96%, N 7.32%, O 8.36%
Literature References: Substituted amide with broad spectrum repellent activity. Prepn: G. Hausknecht, Ber. 22, 324 (1889); R. Mukherjee, J. Chem. Soc. D 1971, 1113; and structure-activity relationship studies: M. V. S. Suryanarayana et al., J. Pharm. Sci. 80, 1055 (1991). Comparative studies with deet and dimethyl phthalate, q.q.v., vs mosquitoes, black flies and land leeches: S. Kumar et al., Indian J. Med. Res. 80, 541 (1984); vs bedbugs: idem et al., ibid. 102, 20 (1995); vs rat flea: K. K. Mathur et al., ibid. 83, 466 (1986); vs sandflies: M. Kalyanasundaram et al., Med. Vet. Entomol. 8, 68 (1994). Comparison with deet and dibutyl phthalate, q.q.v., in prevention of scrub typhus: R. Tilak et al., Indian J. Med. Res. 113, 98 (2001). GC determn in urine: S. S. Rao et al., J. Chromatogr. B 493, 210 (1989). Toxicity and metabolism studies: idem. et al., Toxicology 58, 81 (1989); idem et al., Toxicol. Lett. 45, 67 (1989). Development of polysiloxane based slow release formulations and efficacy vs mosquitoes : D. C. Gupta et al., J. Polym. Mater. 17, 215 (2000). Review: S. S. Rao, K. M. Rao, J. Med. Entomol. 28, 303-306 (1991).

Metoclopramide CAS Registry Number: 364-62-5 甲氧氯普胺

CAS Name: 4-Amino-5-chloro-N-[(2-diethylamino)ethyl]-2-methoxybenzamide
Additional Names: 4-amino-5-chloro-N-[2-(diethylamino)ethyl]-o-anisamide; 4-amino-5-chloro-2-methoxy-N-(b-diethylaminoeth...
Literature References: Substituted benzamide with neuroleptic activity. Prepn: BE 620543; Thominet, US 3177252 (1962, 1965 to Soc. d'Etudes Sci. Ind. de l'Ile-de-France); R. Pakula et al., Arch. Pharm. 313, 297 (1980). Colorimetric determn in plasma and solubility: G. Pitel, T. Luce, Ann. Pharm. Fr. 23, 673 (1965). Dopamine D2 receptor antagonist (adenylate cyclase independent receptors): J. W. Kebabian, D. B. Calne, Nature 277, 93 (1979). Pharmacology: M. A. Smith, F. J. Salter, Drug Intell. Clin. Pharm. 14, 169 (1980). Pharmacokinetics: H. Vergin et al., Arzneim.-Forsch. 33, 458 (1983). Review of efficacy in psychiatric disorders: E. D. Peselow, M. Stanley, Adv. Biochem. Psychopharmacol. 35, 163-194 (1982); of pharmacology and clinical use: R. A. Harrington et al., Drugs 25, 451-494 (1983); ibid., Suppl. 1, 1-88. Comprehensive description: D. Pitré, R. Stradi, Anal. Profiles Drug Subs. 16, 327-361 (1987).

Clenbuterol CAS Registry Number: 37148-27-9 克伦特罗

CAS Name: 4-Amino-3,5-dichloro-a-[[(1,1-dimethylethyl)amino]methyl]benzenemethanol
Additional Names: 4-amino-a-[(tert-butylamino)methyl]-3,5-dichlorobenzyl alcoholTrademarks: Monores (Valeas) Literature References: Substituted phenylethanolamine with b2 sympathomimetic activity. Prepn: J. Keck et al., ZA 6705692; eidem, US 3536712 (1968, 1970 both to Thomae); eidem, Arzneim.-Forsch. 22, 861 (1972). Series of articles on pharmacology, reproductive toxicology, pharmacokinetics and metabolism: ibid. 26, 1403-1419, 1427-1460 (1976). Toxicity: M. Ueberberg et al., ibid. 1420. Clinical studies: M. Tschan et al., Eur. J. Clin. Pharmacol. 15, 159 (1979); C. Pasotti et al., Int. J. Clin. Pharmacol. Biopharm. 17, 176 (1979). Effect on weight gain in lambs: M. E. Nichols et al., 1991 Animal Science Research Report (Oklahoma Agric. Exp. Station, Oklahoma State University, 1991) 303.

Cladribine CAS Registry Number: 4291-63-8 克拉利宾

CAS Name: 2-Chloro-2'-deoxyadenosine
Additional Names: 2-chloro-6-amino-9-(2-deoxy-b-D-erythro-pentofuranosyl)purine; 2-chlorodeoxyadenosine; 2-CdA; CldAdoTrademarks: Leustatin (Ortho Biotech)<...
Literature References: Substituted purine nucleoside with antileukemic activity. Prepn as intermediate in synthesis of 2-deoxynucleosides: H. Venner, Ber. 93, 140 (1960); M. Ikehara, H. Tada, J. Am. Chem. Soc. 85, 2344 (1963); eidem, ibid. 87, 606 (1965). Synthesis and biological activity: L. F. Christensen et al., J. Med. Chem. 15, 735 (1972). Stereospecific synthesis: Z. Kazimierczuk et al., J. Am. Chem. Soc. 106, 6379 (1984); R. K. Robins, G. R. Revankar, EP 173059; eidem, US 4760137 (1986, 1988 both to Brigham Young Univ.). Specific toxicity to lymphocytes: D. A. Carson et al., Proc. Natl. Acad. Sci. USA 77, 6865 (1980); eidem, Blood 62, 737 (1983). Mechanism of action: S. Seto et al., J. Clin. Invest. 75, 377 (1985). Clinical evaluation in chronic lymphocytic leukemia: L. D. Piro et al., Blood 72, 1069 (1988); in hairy cell leukemia: eidem, N. Engl. J. Med. 322, 1117 (1990).

Edoxudine CAS Registry Number: 15176-29-1 乙去氧尿啶

CAS Name: 2'-Deoxy-5-ethyluridine
Additional Names: 5-ethyl-2'-deoxyuridine; 5-ethyl-3-(2'-deoxyribosyl)uracil; EDU; EUDRTrademarks: Aedurid (Robugen); Edurid (Robugen)
Percent Composition: ...
Literature References: Substituted uracil with anti-herpes activity. Prepn and properties: K. K. Gauri, GB 1170565; eidem, US 3553192 (1968, 1971 both to Robugen). Synthesis via organopalladium intermediates: D. E. Bergstrom, J. L. Ruth, J. Am. Chem. Soc. 98, 1587 (1976); D. E. Bergstrom, M. K. Ogawa, ibid. 100, 8106 (1978). Physical properties: M. Swierkowski, D. Shugar, J. Med. Chem. 12, 533 (1969). Antiviral activity: E. De Clercq, D. Shugar, Biochem. Pharmacol. 24, 1073 (1975). Preferential inhibition of herpes simplex virus type 2: C.-Z. Teh, S. L. Sacks, Antimicrob. Agents Chemother. 23, 637 (1983). Synergistic effect with interferon-b, q.v., on herpes simplex virus: C. Janz, R. Wigand, Arch. Virol. 73, 135 (1982). Inhibitory effect on growth of murine leukemia cells: J. Balzarini et al., Invest. New Drugs 2, 35 (1984).

Desosamine CAS Registry Number: 5779-39-5 脱氧氨基糖

CAS Name: 3,4,6-Trideoxy-3-(dimethylamino)-D-xylo-hexose
Additional Names: 4-dimethylaminotetrahydro-6-methylpyran-2,3-diol; picrocine
Percent Composition: C 54.83%, H 9.78%, N 7.99%, O 27.3...
Literature References: Sugar component of several macrolide antibiotics, such as the erythromycins. Isoln: Clark, Antibiot. Chemother. 3, 663 (1953). Identity with picrocine: Brockmann et al., Ber. 87, 856 (1954). Stereochemistry: Woo et al., Tetrahedron Lett. 1962, 735. Configuration: Bolton et al., Chem. Ind. (London) 1962, 1945; Foster et al., J. Chem. Soc. 1965, 2318. Synthesis of DL-form: Korte et al., Tetrahedron 18, 657 (1962); Newman, Chem. Ind. (London) 1963, 372; J. Org. Chem. 29, 1461 (1964). Stereospecific synthesis of the natural D-form: Richardson, J. Chem. Soc. 1964, 5364; of the L-form: Baer, Chiu, Can. J. Chem. 52, 122 (1974).

Tevenel® (Midy Labs) CAS Registry Number: 4302-95-8 氨枫霉素

CAS Name: N-[(1R,2R)-2-[4-(Aminosulfonyl)phenyl]-2-hydroxy-1-(hydroxymethyl)ethyl]-2,2-dichloroacetamide
Additional Names: D-threo-(-)-2,2-dichloro-N-[b-hydroxy-a-(hydroxymethyl)-p-sulfamoylphe...
Literature References: Sulfamoyl analog of chloramphenicol. Prepn: Gregory, US 2680135 (1954 to Du Pont). Toxicology: R. M. Jiji et al., Arch. Int. Med. 111, 70 (1963).

CHAPS CAS Registry Number: 75621-03-3 3-[(3-胆固醇氨丙基)二甲基氨基]-1-丙磺酸

CAS Name: N,N-Dimethyl-N-(3-sulfopropyl)-3-[[(3a,5b,7a,12a)-3,7,12-trihydroxy-24-oxocholan-24-yl]amino]-1-propanaminium inner salt
Additional Names: 3-[(3-cholamidopropyl)dimethylammonio]-1-pro...
Literature References: Sulfobetaine zwitterionic derivative of cholic acid, q.v. Prepn: L. M. Hjelmeland, Proc. Natl. Acad. Sci. USA 77, 6368 (1980); idem, US 4372888 (1983 to U.S. Secy. Health and Human Services); and physical properties: L. M. Hjelmeland et al., Anal. Biochem. 130, 72 (1983). Physical characterization: R. E. Stark et al., J. Phys. Chem. 88, 6063 (1984). Micellar properties: M. A. Partearroyo et al., Biochem. Int. 16, 259 (1988). Solubilization of membrane proteins: A. J. Bitonti et al., Biochemistry 21, 3650 (1982); W. Wouters et al., Eur. J. Pharmacol. 115, 1 (1985); L. Bancells et al., Biochem. Pharmacol. 36, 2539 (1987); of opioid receptors: J. Simon et al., J. Neurochem. 46, 695 (1986).

Zonisamide CAS Registry Number: 68291-97-4 唑尼沙胺

CAS Name: 1,2-Benzisoxazole-3-methanesulfonamide
Additional Names: 3-(sulfamoylmethyl)-1,2-benzisoxazoleTrademarks: Excegran (Dainippon); Zonegran (Dainippon)
Percent Composition: C 45.27%, ...
Literature References: Sulfonamide antiseizure agent; blocks repetitive firing of voltage-sensitive sodium channels and reduces voltage-sensitive T-type calcium currents. Prepn: H. Uno et al., JP Kokai 78 77057; eidem, US 4172896 (1978, 1979 both to Dainippon); eidem, J. Med. Chem. 22, 180 (1979). Pharmacology and toxicity: Y. Masuda et al., Arzneim.-Forsch. 30, 477 (1980). Mode of action study: T. Ito et al., ibid. 603. HPLC determn in serum: U. Juergens, J. Chromatogr. 385 233 (1987). Clinical trial in epilepsy: D. Schmidt et al., Epilepsy Res. 15, 67 (1993). Review of neuropharmacology: E. J. Hammond et al., Gen. Pharmacol. 18, 303 (1987); of pharmacokinetics and therapeutic potential: D. H. Peters, E. M. Sorkin, Drugs 45, 760-787 (1993); of pharmacokinetics and mechanism of action: I. E. Leppik, Seizure 13S, S5-S9 (2004).