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

Bimosiamose CAS Registry Number: 187269-40-5 比莫西糖

CAS Name: 3',3'''-(1,6-Hexanediyl)bis[6'-(a-D-mannopyranosyloxy)[1,1'-biphenyl]]-3-acetic acid
Additional Names: 1,6-bis[3-(3-carboxymethylphenyl)-4-(2-a-D-mannopyranosyloxy)phenyl]hexanePercen...
Literature References: Pan-selectin receptor antagonist. Prepn: T. P. Kogan et al., WO 9701335; eidem, US 5919768 (1997, 1999 both to Texas Biotechnol.); eidem, J. Med. Chem. 41, 1099 (1998). Stereospecific synthesis: I. L. Scott et al., Carbohydr. Res. 317, 210 (1999). Review of pharmacology and clinical development: L. Pradella, Curr. Opin. Anti-Inflam. Immunomod. Invest. Drugs 1, 56-60 (1999); E. Aydt, G. Wolff, Pathobiology 70, 297-301 (2003). Clinical pharmacokinetics: M. Meyer et al., Int. J. Clin. Pharmacol. Ther. 43, 463 (2005). Clinical evaluation in allergic asthma: K. M. Beeh et al., Pulm. Pharmacol. Ther. 19, 233 (2006).

Atropine CAS Registry Number: 51-55-8 阿托品; 颠茄碱

CAS Name: a-(Hydroxymethyl)benzeneacetic acid (3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester
Additional Names: 1aH,5aH-tropan-3a-ol (±)-tropate (ester); dl-hyoscyamine; tropic acid es...
Literature References: Parasympatholytic alkaloid isolated from Atropa belladonna L., Datura stramonium L., and other Solanaceae. Extraction procedure: Chemnitius, J. Prakt. Chem. 116, 276 (1927). During extraction, partial racemization of the l-hyoscyamine takes place which is completed by treatment with dil alkali on heating in chloroform soln: Schneider, Arch. Pharm. 284, 306 (1951). Structure and synthesis: Ladenburg, Ann. 217, 75 (1883); Willstätter, Ber. 31, 1537 (1898); idem., Ann. 326, 23 (1903); Schwenker et al., Ber. 99, 2407 (1966). Prepn of the sulfate: DE 247455 (1912 to Hoffmann-La Roche), Frdl. 11, 1022. Use as antidote to cholinesterase inhibitors: R. V. Brown, Br. J. Pharmacol. 15, 170 (1960). Effect on cardiac arrhythmias: P. Schweitzer, H. Mark, Am. Heart J. 100, 119, 255 (1980). Pharmacokinetics and pharmacodynamics: P. H. Hinderling et al., J. Pharm. Sci. 74, 703, 711 (1985). Toxicity: R. L. Cahen, K. Tvede, J. Pharmacol. Exp. Ther. 105, 166 (1952); Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Review of clinical use in anesthesia: L. E. Shutt, J. B. Bowes, Anaesthesia 34, 476-490 (1979). Comprehensive description: A. A. Al-Badr, F. J. Muhtadi, Anal. Profiles Drug Subs. 14, 325-389 (1985). Review of clinical toxicology: J. D. Truwit, Crit. Care Clin. 7, 639-657 (1991).

Carbachol CAS Registry Number: 51-83-2 卡巴胆碱

CAS Name: 2-[(Aminocarbonyl)oxy]-N,N,N-trimethylethanaminium chloride
Additional Names: (2-hydroxyethyl)trimethyl ammonium chloride carbamate; choline chloride carbamate; carbamylcholine chlori...
Literature References: Parasympathomimetic. Prepn: O. Dalmer, C. Diehl, DE 539329 (1930 to E. Merck); eidem, US 1894162 (1933); Kreitmair, Arch. Exp. Pathol. Pharmakol. 164, 346 (1932); R. D. Haworth et al., J. Chem. Soc. 1947, 176. Toxicity: Molitor, J. Pharmacol. Exp. Ther. 58, 337 (1936). Evaluation in bronchoprovocation test for asthma: G. Rosati et al., Eur. J. Respir. Dis. 64, Suppl. 128, 417 (1983). Clinical effect on post-surgical intraocular pressure: R. S. Ruiz et al., Am. J. Ophthalmol. 107, 7 (1989).

Isolysergic Acid CAS Registry Number: 478-95-5 D-异麦角酸

CAS Name: (8a)-9,10-Didehydro-6-methylergoline-8-carboxylic acid
Percent Composition: C 71.62%, H 6.01%, N 10.44%, O 11.93%
Literature References: Parent compd of the ergotinine group of alkaloids from ergot. Prepn: Smith, Timmis, J. Chem. Soc. 1936, 1440; Craig et al., J. Biol. Chem. 125, 289 (1938). Differs from lysergic acid by the a-configuration at C-8. Stereochemical studies: Stenlake, J. Chem. Soc. 1955, 1626; Leemann, Fabbri, Helv. Chim. Acta 42, 2696 (1959).

Gephyrotoxin CAS Registry Number: 55893-12-4 桥虫毒素

CAS Name: (1R,3aR,5aR,6R,9aS)-Dodecahydro-6-(2Z)-2-penten-4-ynyl-pyrrolo[1,2-a]-quinoline-1-ethanol
Additional Names: HTX D; histrionicotoxin D
Percent Composition: C 79.39%, H 10.17%, N 4.8...
Literature References: Parent member of a class of tricyclic perhydrobenzoindolizine neurotoxin alkaloids isolated from the skin secretions of the Colombian poison-dart frogs Dendrobates histrionicus and Dendrobates occultator, family Dendrobatidae. The name gephyrotoxin was coined from the Greek word "gephyra" meaning "bridge", and refers to the bridge presumably formed by addition of the nitrogen function to one side of a 2,6-disubstituted piperidine precursor to form the bicyclic indolizine. Isolation of naturally occurring l-form: T. Tokuyama et al., Helv. Chim. Acta 57, 2597 (1974). Structure and absolute configuration: J. W. Daly et al., ibid. 60, 1128 (1977). Revised configuration: R. Fujimoto, Y. Kishi, Tetrahedron Lett. 1981, 4197. Total synthesis of (±)-form: R. Fujimoto et al., J. Am. Chem. Soc. 102, 7154 (1980); D. J. Hart, J. Org. Chem. 46, 3576 (1981); D. J. Hart, K. Kanai, J. Am. Chem. Soc. 105, 1255 (1983); L. E. Overman et al., ibid. 5373. Complete proton and 13C NMR assignment: M. W. Edwards, A. Bax, ibid. 108, 918 (1986). Effect on neuromuscular transmission: C. Souccar et al., Mol. Pharmacol. 25, 384, 395 (1984). Receptor binding study: R. S. Aronstam et al., Neurochem. Res. 11, 1227 (1986). Review including discussion of gephyrotoxin congeners: J. W. Daly, Fortschr. Chem. Org. Naturst. 41, 283-300 (see also refs pp 326-340) (1982).

Ceftriaxone CAS Registry Number: 73384-59-5 头孢曲松

CAS Name: (6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)(methoxyimino)acetyl]amino]-8-oxo-3-[[(1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl)thio]methyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-c...
Literature References: Parenteral third generation cephalosporin antibiotic. Prepn: M. Montavon, R. Reiner, GB 2022090; eidem, US 4327210 (1979, 1982 both to Hoffmann-La Roche); R. Reiner et al., J. Antibiot. 33, 783 (1980). In vitro and in vivo studies: P. Angehrn et al., Antimicrob. Agents Chemother. 18, 913 (1980). Pharmacokinetics: M. Seddon et al., ibid. 240. Determn in plasma, urine, bile: K. H. Trautmann, P. Haefelfinger, J. High Resolut. Chromatogr. Chromatogr. Commun. 4, 54 (1981), C.A. 94, 202437 (1981). Mechanism of action study: R. B. Wright et al., J. Antibiot. 34, 590 (1981). Kinetics in humans: K. Stoekel et al., Clin. Pharmacol. Ther. 29, 650 (1981). Toxicity data: K. Teelman et al., "Experimentelle Toxikologie von Ceftriaxon", in Ceftriaxon ein neues parenterales Cephalosporin, Proc. Hahnenklee Symp., 1981, R. Grieshalber, Ed. (Editiones Roche, Basel, 1982) pp 91-111. Review of antibacterial activity, toxicology, pharmacology and clinical studies: D. M. Richards et al., Drugs 27, 469 (1984); T. R. Beam, Pharmacotherapy 5, 237-253 (1985).

Mycaminose CAS Registry Number: 519-21-1 碳霉氨糖

CAS Name: 3,6-Dideoxy-3-(dimethylamino)-D-glucose
Percent Composition: C 50.25%, H 8.96%, N 7.32%, O 33.47%
Literature References: Part of the carbomycin molecule. Synthesis and stereochemistry: Richardson, Proc. Chem. Soc. London 1961, 430; Foster et al., Chem. Ind. (London) 1962, 142. Stereochemistry: Grisebach, Hofheinz, Angew. Chem. 74, 499 (1962).

Rabeprazole CAS Registry Number: 117976-89-3 雷贝拉唑

CAS Name: 2-[[[4-(3-Methoxypropoxy)-3-methyl-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazole
Additional Names: pariprazole
Percent Composition: C 60.15%, H 5.89%, N 11.69%, O 13.35%, S 8.92%
Literature References: Partially reversible gastric proton pump inhibitor. Prepn: S. Souda et al., EP 268956; eidem, US 5045552 (1988, 1991 both to Eisai). Pharmacology: H. Goto et al., Arzneim.-Forsch. 41, 635 (1991). Mode of action: M. Morii, N. Takeguchi, J. Biol. Chem. 268, 21553 (1993). HPLC determn in plasma: H. Nakai et al., J. Chromatogr. B 660, 211 (1994). Clinical pharmacokinetics: S. Yasuda et al., Int. J. Clin. Pharmacol. Ther. 32, 466 (1994). Review of clinical trials in acid peptic diseases: M. L. Cloud et al., Dig. Dis. Sci. 43, 993-1000 (1998); of pharmacology and clinical experience in gastro-esophageal reflux disease: B. Thjodleifsson, Expert Opin. Pharmacother. 5, 137-149 (2004).

Urea Stibamine CAS Registry Number: 1340-35-8 (4-氨基苯基)-(氨基甲酰氨基)氧基次锑酸

Additional Names: Carbostibamide
Literature References: Pentavalent antimonial. Therapeutic efficacy in kala-azar: U. N. Brahmachari, Indian J. Med. Res. 10, 492 (1922). Prepn and proposed structure as NH2CONHC6H4SbO(OH)ONH4: U. N. Brahmachari, J. Das, ibid. 12, 423 (1924). Shown to be a mixture of products with sym-diphenylcarbamido-4,4¢-distibonic acid as the active principal: W. H. Gray et al., Proc. Roy. Soc. B108, 54 (1931). Description of development: R. C. Guha et al., Nature 151, 108 (1943); W. Peters, Indian J. Med. Res. 73 Suppl., 1 (1981). Improved prepn, characterization and activity: S. B. Mahato et al., Biochem. Med. Metab. Biol. 38, 47 (1987).

Acetarsone CAS Registry Number: 97-44-9 阿西太松

CAS Name: [3-(Acetylamino)-4-hydroxyphenyl]arsonic acid
Additional Names: N-acetyl-4-hydroxy-m-arsanilic acid; 3-acetamido-4-hydroxyphenylarsonic acid; 3-acetamido-4-hydroxybenzenearsonic acid;...
Literature References: Pentavalent arsenical formerly used in the treatment of syphilis. Also used in combination with arecoline, q.v. Prepn: Raiziss, Fisher, J. Am. Chem. Soc. 48, 1323 (1926); Hewitt, King, J. Chem. Soc. 1926, 823. Toxicity data: H. H. Anderson, C. D. Leake, Proc. Soc. Exp. Biol. Med. 27, 267 (1930).