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

Pilocarpine CAS Registry Number: 92-13-7 毛果芸香碱

CAS Name: (3S-cis)-3-Ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2(3H)-furanone
Trademarks: Ocusert Pilo (Cusi)
Percent Composition: C 63.44%, H 7.74%, N 13.45%, O 15.36%
Literature References: Cholinergic principle from Pilocarpus jaborandi Holmes, Rutaceae. Isoln: Petit, Polanovski, Bull. Soc. Chim. [3] 17, 557, 702 (1897). Structure: Jowett, J. Chem. Soc. 77, 473, 851 (1900); 83, 438 (1903). Stereoisomeric with isopilocarpine: Polonovski, Polonovski, Bull. Soc. Chim. [4] 31, 1314 (1922). Has the cis configuration; isopilocarpine is trans: Zav'yalov, Dokl. Akad. Nauk SSSR 82, 257 (1952). Absolute configuration: Hill, Barcza, Tetrahedron 22, 2889 (1966). Synthesis: Preobrashenski et al., Ber. 66, 1187 (1933); Samokhvalov, Med. Prom. SSSR 11, no. 2, 10 (1957); DeGraw, Tetrahedron 28, 967 (1972); Link, Bernauer, Helv. Chim. Acta 55, 1053 (1972). Stereoselective synthesis: A. Noordam et al., Rec. Trav. Chim. 98, 467 (1979). Review: Langenbeck, Angew. Chem. 60, 297 (1948); van Rossum et al., Experientia 16, 373 (1960). Toxicity studies: Beccari, Boll. Chim. Farm. 106, 8 (1967). Comprehensive description: A. A. Al-Badr, H. Y. Aboul-Enein, Anal. Profiles Drug Subs. 12, 385-432 (1983). Clinical trial in Sjögren's syndrome: F. B. Vivino et al., Arch. Intern. Med. 159, 174 (1999); in radiation-induced xerostomia: J.-C. Horiot et al., Radiother. Oncol. 55, 233 (2000).

Methyl Demeton CAS Registry Number: 8022-00-2 甲基内吸磷

CAS Name: Phosphorothioic acid O-[2-(ethylthio)ethyl] O,O-dimethyl ester mixt with S-[2-(ethylthio)ethyl] O,O-dimethyl phosphorothioate
Additional Names: demeton-methyl; methyl-mercaptophos; me...
Literature References: Cholinesterase inhibitor. Isomeric mixture consisting of demeton-O-methyl and demeton-S-methyl (O(and S)-[2-(ethylthio)ethyl] O,O-dimethyl phosphorothioate). Ref: Henglein, Schrader, Z. Naturforsch. 10b, 12 (1955). Prepn: GB 814332 (1959 to Bayer). Toxicology studies: M. Vandekar, Br. J. Ind. Med. 15, 158 (1958); E. F. Edson, Pharm. J. 185, 361 (1960).

Edrophonium Chloride CAS Registry Number: 116-38-1 依酚氯铵

CAS Name: N-Ethyl-3-hydroxy-N,N-dimethylbenzenaminium chloride
Additional Names: ethyl(m-hydroxyphenyl)dimethylammonium chloride; (3-hydroxyphenyl)dimethylethylammonium chloride; 3-hydroxy-N,N-...
Literature References: Cholinesterase inhibitor. Prepn: J. A. Aeschlimann, A. Stempel, US 2647924 (1953 to Hoffmann-La Roche). LC determn in biological fluids: M. G. M. DeRuyter et al., J. Chromatogr. 183, 193 (1980). Clinical evaluation in reversal of neuromuscular blockade: D. M. Fisher et al., Anesthesiology 61, 428 (1984). Clinical study in supraventricular tachycardia: J. D. Cantwell et al., Arch. Int. Med. 130, 221 (1972). Diagnostic use in myasthenia gravis: I. M. Williams et al., Clin. Exp. Neurol. 22, 1 (1986); in esophageal chest pain: C. A. Lee et al., Dig. Dis. Sci. 32, 682 (1987).

Eptastigmine CAS Registry Number: 101246-68-8 依斯的明

CAS Name: (3aS,8aR)-1,2,3,3a,8,8a-Hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-yl heptylcarbamic acid ester
Additional Names: N-demethyl-N-heptylphysostigmine; heptylphysostigmine; heptylsti...
Literature References: Cholinesterase inhibitor; analog of physostigmine, q.v. Prepn: M. Pomponi et al., EP 154864; M. Brufani et al., US 4831155 (1985, 1989 both to Consiglio Naz. Ricerche). Prepn of tartrate: P. G. Pagella et al., EP 298202 (1989 to Mediolanum Farm. and Consiglio Naz. Ricerche). Prepn and pharmacology: M. Marta et al., Life Sci. 43, 1921 (1988). Anticholinesterase activity: P. De Sarno et al., Neurobiochem. Res. 14, 971 (1989). Clinical cholinesterase inhibition: L. K. Unni et al., Eur. J. Clin. Pharmacol. 41, 83 (1991).

Ipidacrine CAS Registry Number: 62732-44-9 2,3,5,6,7,8-六氢-1H-环戊并[b]喹啉-9-胺

CAS Name: 2,3,5,6,7,8-Hexahydro-1H-cyclopenta[b]quinolin-9-amine
Additional Names: 9-amino-2,3,5,6,7,8-hexahydro-1H-cyclopenta[b]quinoline; amiridin
Percent Composition: C 76.55%, H 8.57%, N...
Literature References: Cholinesterase inhibitor; structural analog of tacrine. Prepn: A. V. Upadysheva et al., Khim. Farm. Zh. 11, 40 (1977), C.A. 86, 189676q (1977). Prepn of the hydrochloride monohydrate: E. F. Levretskaya et al., DE 3231571; eidem, US 4550113 (1984, 1985 both to Sci. Res. Inst. Biol. Test. Chem. Compds). Neuropharmacology: T. Nabeshima et al., Eur. J. Pharmacol. 154, 263 (1988). Anticholinesterase activity: S. Shibanoki et al., Pharmacol. Biochem. Behav. 39, 499 (1991). Clinical evaluation in Alzheimer's disease: E. E. Bukatina et al., Neurosci. Behav. Physiol. 23, 83 (1993).

Pralidoxime Chloride CAS Registry Number: 51-15-0 氯解磷定

CAS Name: 2-[(Hydroxyimino)methyl]-1-methylpyridinium chloride
Additional Names: 2-formyl-1-methylpyridinium chloride oxime; 1-methyl-2-formylpyridinium chloride oxime; N-methylpyridinium-2-ald...
Literature References: Cholinesterase reactivator. Prepn of salts: I. B. Wilson et al., US 2816113 (1957 to U.S. Sec'y. of Army); A. A. Kondritzer et al., J. Pharm. Sci. 50, 109 (1961). Manufacturing processes: R. I. Ellin et al., US 3140289 (1964 to U.S. Dept. of the Army); McDowell, US 3155674 (1964 to Olin Mathieson). Commercial prepn: R. I. Ellin, Ind. Eng. Chem. Prod. Res. Dev. 3 (1), 20 (1964). HPLC determn in serum: P. Houzé et al., J. Chromatogr. B 814, 149 (2005). Toxicology: Christensen, Richter, Arch. Environ. Health 15, 599 (1967). Toxicity data: Fleisher et al., Toxicol. Appl. Pharmacol. 16, 40 (1970); R. I. Ellin, J. H. Wills, J. Pharm. Sci. 53, 1143 (1964). Comprehensive description: U. V. Banakar, U. N. Patel, Anal. Profiles Drug Subs. 17, 533-569 (1988).

Asoxime Chloride CAS Registry Number: 34433-31-3; 124051-64-5 (free base)

CAS Name: 1-[[[4-(Aminocarbonyl)pyridinio]methoxy]methyl]-2-[(hydroxyimino)methyl]pyridinium dichloride
Additional Names: 4'-carbamoyl-2-formyl-1,1'-(oxydimethylene)dipyridinium chloride 2-oxim...
Literature References: Cholinesterase reactivator. Prepn: I. Hagedorn, US 3773775 (1973 to E. Merck); L. Y. Y. Hsiao, H. A. Musallam, US 5130438 (1992 to U.S.A. Secy. of Army). Chemical stability study: P. Eyer et al., Arch. Toxicol. 59, 266 (1986). Dissolution properties: H. Thiermann et al., Int. J. Pharm. 137, 167 (1996). HPLC determn in plasma: M. P. McCluskey et al., J. Anal. Toxicol. 14, 239 (1990). Metabolism study: D. J. Ecobichon et al., Can. J. Physiol. Pharmacol. 68, 614 (1990). Clinical pharmacokinetics and safety: J. G. Clement et al., Biopharm. Drug Dispos. 16, 415 (1995). Clinical evaluation in insecticide poisoning: R. Kusic et al., Hum. Exp. Toxicol. 10, 113 (1991). Review of pharmacology: C. G. Rousseaux, A. K. Dua, Can. J. Physiol. Pharmacol. 67, 1183-1189 (1989); of physical properties and acute toxicity: J. G. Clement et al., Arch. Toxicol. 62, 220-223 (1988).

Besipirdine CAS Registry Number: 119257-34-0 贝西吡啶

CAS Name: N-Propyl-N-4-pyridinyl-1H-indol-1-amine
Additional Names: 1-(propyl-4-pyridylamino)indole
Percent Composition: C 76.46%, H 6.82%, N 16.72%
Literature References: Cholinomimetic agent with noradrenergic activity. Prepn: R. C. Effland, J. T. Klein, EP 287982 (1988 to Hoechst); idem et al., US 4970218 (1990 to Hoechst-Roussel); of hydrochloride: S. Kongsamut et al., US 5356910 (1994 to Hoechst-Roussel). HPLC determn in plasma: R. S. Hsu et al., J. Chromatogr. 572, 352 (1991). Mechanism of action study: C. P. Smith et al., Drug Dev. Res. 32, 13 (1994). Pharmacokinetics: J. W. Hubbard et al., J. Clin. Pharmacol. 35, 688 (1995).

Nitrocefin CAS Registry Number: 41906-86-9 头孢硝噻吩

CAS Name: (6R,7R)-3-[(1E)-2-(2,4-Dinitrophenyl)ethenyl]-8-oxo-7-[(2-thienylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: 3-(2,4-dinitrostyryl)-(6R,7R)-7-...
Literature References: Chromogenic cephalosporin. Prepd (not claimed): C. H. O'Callaghan et al., US 3830700 (1974 to Glaxo). Characterization and use in detection of b-lactamases: idem et al., Antimicrob. Agents Chemother. 1, 283 (1972). Synthesis: N. C. M. Barendse et al., Synthesis 1998, 145. Improved synthesis: M. Lee et al., J. Org. Chem. 70, 367 (2005). Review of commercially available nitrocefin-based b-lactamase tests: A. T. Meszaros et al., Am. Clin. Lab. 14, 20-22 (1995).

X-gal CAS Registry Number: 7240-90-6 5-溴-4-氯-3-吲哚半乳糖苷

CAS Name: 5-Bromo-4-chloro-1H-indol-3-yl b-D-galactopyranoside
Percent Composition: C 41.15%, H 3.70%, Br 19.55%, Cl 8.68%, N 3.43%, O 23.49%
Literature References: Chromogenic substrate of the lacZ gene product, b-galactosidase; produces a rich blue color when cleaved by the enzyme. Prepn: J. P. Horwitz et al., J. Med. Chem. 7, 574 (1964). Colorimetric reaction in tissue to localize b-galactosidase: B. Pearson et al., Lab. Invest. 12, 1249 (1963); Z. Lojda, Histochemie 23, 266 (1970). Protocol for blue-white a-complementation screening: J. Sambrook et al., Molecular Cloning: A Laboratory Manual (Cold Spring Harbor, New York, 2nd ed., 1989) pp 1.7-1.9, 1.85-1.87. Optimization of detection of exogenous bacterial lacZ expression: D. J. Weiss et al., Hum. Gene Ther. 8, 1545 (1997); of fixative conditions in X-gal staining: W. Ma et al., J. Histochem. Cytochem. 50, 1421 (2002); of blue-white screening procedure: A. L. Sherwood, BioTechniques 34, 644 (2003).