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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

  • Enalaprilat CAS Registry Number: 76420-72-9 依那普利拉


    CAS Name: N-[(1S)-1-Carboxy-3-phenylpropyl]-L-alanyl-L-proline dihydrate
    Additional Names: enalaprilic acidTrademarks: Vasotec IV (Merck Co.)
    Percent Composition: C 56.24%, H 7.34%, N 7.29%...
    Literature References: Nonsulfhydryl dipeptide angiotensin converting enzyme (ACE) inhibitor. Prepn: A. A. Patchett et al., Nature 288, 280 (1980); eidem, EP 12401; E. E. Harris et al., US 4374829 (1980, 1983 both to Merck Co.). Active metabolite of enalapril, q.v.: D. J. Tocco et al., Drug Metab. Dispos. 10, 15 (1982). Pharmacology: D. M. Gross et al., J. Pharmacol. Exp. Ther. 216, 552 (1981); M. A. Nelson et al., Clin. Exp. Pharmacol. Physiol. Suppl. 7, 87 (1982); T. A. Unger et al., Biochem. Pharmacol. 31, 3063 (1982). Bioavailability: M. L. Cohen et al., J. Pharmacol. Exp. Ther. 226, 192 (1983). Kinetics of enzyme inhibition: C. H. Reynolds, Biochem. Pharmacol. 33, 1273 (1984). Pharmacokinetics: K. S. Pang et al., Drug Metab. Dispos. 12, 309 (1984). Acute hemodynamic effects in essential hypertension: A. C. Simon et al., Clin. Pharm. Ther. 43, 49 (1988). Clinical evaluation in severe and malignant hypertension: D. J. DiPette et al., ibid. 38, 199 (1985).

  • Repaglinide CAS Registry Number: 135062-02-1 瑞格列奈


    CAS Name: 2-Ethoxy-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzoic acid
    Additional Names: (+)-2-ethoxy-a-[[(S)-a-isobutyl-o-piperidinobenzyl]carbamoyl]-p-toluic ...
    Literature References: Non-sulfonylurea oral hypoglycemic agent. Prepn: W. Grell et al., WO 9300337 (1993 to Thomae). HPLC determn of racemate in human plasma: A. Greischel et al., J. Chromatogr. 568, 246 (1991). Clinical pharmacokinetics: F. J. Ampudia-Blasco et al., Diabetologia 37, 703 (1994). Comparative clinical evaluation in NIDDM: B. H. R. Wolffenbuttel et al., Eur. J. Clin. Pharmacol. 45, 113 (1993).

  • Trinitrotriazidobenzene CAS Registry Number: 29306-57-8 1,3,5-三叠氮基-2,4,6-三硝基苯


    CAS Name: 1,3,5-Triazido-2,4,6-trinitrobenzene
    Additional Names: TNTA
    Percent Composition: C 21.44%, N 50.00%, O 28.56%
    Literature References: Nontoxic, metal-free, high energy density material. Explodes to produce gaseous nitrogen and carbon dioxide. Prepn: I. O. Turek, Chim. Ind. (Paris) 26, 785 (1931). Use as a fixative in immunofluorescence microscopy: E. McBeath, K. Fujiwara, J. Cell Biol. 99, 2061 (1984). Thermal decompn studies: A. D. Yoffe, Proc. R. Soc. London Ser. A 208, 188 (1951); D. Adam et al., Heteroatom Chem. 10, 548 (1999). Synthesis, crystal structure, and detonation properties: idem et al., Propellants Explosives Pyrotechnics 27, 7 (2002).

  • Oxaflozane CAS Registry Number: 26629-87-8 丙吗啉氟苄


    CAS Name: 4-(1-Methylethyl)-2-[3-(trifluoromethyl)phenyl]morpholine
    Additional Names: 4-isopropyl-2-(a,a,a-trifluoro-m-tolyl)morpholine; tetrahydro-4-isopropyl-2-[3-(trifluoromethyl)phenyl]-2H-...
    Literature References: Non-tricyclic antidepressant agent. Prepn: R. Y. Mauvernay et al., FR 1564792; eidem, US 3637680 (1969, 1972 both to CERM); N. Busch et al., Eur. J. Med. Chem. - Chim. Ther. 11, 201 (1976). Improved synthesis: P. M. Weintraub et al., J. Org. Chem. 45, 4989 (1980). Pharmacological profile: J. Hache et al., Therapie 29, 81 (1974). Urinary metabolism: M. Constantin, J. F. Pognat, Arzneim.-Forsch. 29, 109 (1979). Preliminary clinical study: A. Rascol et al., Therapie 29, 95 (1974).

  • Iobenguane CAS Registry Number: 80663-95-2 间碘苯胍硫酸盐


    CAS Name: [(3-Iodophenyl)methyl]guanidine
    Additional Names: m-iodobenzylguanidine; MIBG
    Percent Composition: C 34.93%, H 3.66%, I 46.13%, N 15.28%
    Literature References: Norepinephrine analog with specific affinity for tissues of sympathetic nervous system and related tumors; prepd as 123I and 131I labeled forms. Prepn and imaging studies: D. M. Wieland et al., J. Nucl. Med. 21, 349 (1980); eidem, US 4584187 (1986). Improved synthesis: P. A. P. M. van Doremalen, A. G. M. Janssen, J. Radioanal. Nucl. Chem. Lett. 96, 97 (1985). Metabolism in man: T. J. Mangner et al., J. Nucl. Med. 27, 37 (1986). HPLC determn in serum and urine: D. Schwabe et al., J. Chromatogr. 487, 177 (1989). Radiopharmacokinetics: S. Ertl et al., Nucl. Med. Commun. 8, 643 (1987). Clinical evaluation of myocardial imaging: D. Fagret et al., Eur. J. Nucl. Med. 15, 624 (1989). Diagnostic use in pheochromocytoma: B. Shapiro et al., J. Nucl. Med. 26, 576 (1985); therapeutic use: M. Krempf et al., J. Clin. Endocrinol. Metab. 72, 455 (1991). Symposia on therapeutic and diagnostic use in neuroblastoma: Advances in Neuroblastoma Research 2, A. E. Evans et al., Eds. (Alan R. Liss, Inc., New York, 1988) p 643-726; Med. Pediatr. Oncol. 15, 157-228 (1987). Review of pharmacology: J. C. Sisson, D. M. Weiland, Am. J. Physiol. Imaging 1, 96-103 (1986); of biodistribution and clinical studies: A. R. Wafelman et al., Eur. J. Nucl. Med. 21, 545-559 (1994); of therapeutic use in neural crest tumors: L. Troncone, V. Rufini, Anticancer Res. 17, 1823-1832 (1997).

  • Binedaline CAS Registry Number: 60662-16-0 苯奈达林


    CAS Name: N,N,N'-Trimethyl-N'-(3-phenyl-1H-indol-1-yl)-1,2-ethanediamine
    Additional Names: 1-[[2-(dimethylamino)ethyl]methylamino]-3-phenylindole; binodaline
    Percent Composition: C 77.78%, H...
    Literature References: Norepinephrine reuptake inhibitor with antidepressant activity. Prepn: F. Schatz et al., DE 2512702; eidem, US 4204998 (1975, 1980 both to Siegfried); eidem, Arzneim.-Forsch. 30, 919 (1980). Mechanism of action study: D. P. Benfield, D. K. Luscombe, ibid. 33, 847 (1983). Pharmacology, toxicity: U. Jahn et al., ibid. 726. Biochemical studies: J. Maj et al., ibid. 841. Binding to human plasma proteins: D. Morin et al., J. Pharm. Sci. 74, 727 (1985). Clinical pharmacology: P. H. Joubert et al., Eur. J. Clin. Pharmacol. 27, 667 (1985).

  • Atomoxetine CAS Registry Number: 83015-26-3 托莫西汀


    CAS Name: (gR)-N-Methyl-g-(2-methylphenoxy)benzenepropanamine
    Additional Names: (-)-N-methyl-3-(o-tolyloxy)-3-phenylpropylamine; tomoxetine
    Percent Composition: C 79.96%, H 8.29%, N 5.49%, O...
    Literature References: Norepinephrine reuptake inhibitor. Prepn (stereochem unspec): B. B. Molloy, K. K. Schmiegel, DE 2500110; eidem, US 4314081 (1975, 1982 both to Lilly). Prepn of (R)-form: B. J. Foster, E. R. Lavagnino, EP 52492 (1982 to Lilly); Y. Gao, K. B. Sharpless, J. Org. Chem. 53, 4081 (1988). Clinical pharmacokinetics: N. A. Farid et al., J. Clin. Pharmacol. 25, 296 (1985). Binding study: D. R. Gehlert et al., J. Neurochem. 64, 2792 (1995). Biotransformation by human liver microsomes: B. J. Ring et al., Drug Metab. Dispos. 30, 319 (2002). Evaluation of abuse potential: S. H. Heil et al., Drug Alcohol Depend. 67, 149 (2002). Clinical trial in pediatric ADHD: C. J. Kratochvil et al., J. Am. Acad. Child Adolesc. Psychiatry 41, 776 (2002); and comorbid tic disorders: A. J. Allen et al., Neurology 65, 1941 (2005). Review of clinical pharmacokinetics: J.-M. Sauer et al., Clin. Pharmacokinet. 44, 571-590 (2005).

  • Ptaquiloside CAS Registry Number: 87625-62-5 (2'R,3a'R,4'S,7a'R)-4'-羟基-2',4',6'-三甲基-3'-氧代-2',3',3a',4'-四氢螺[环丙烷-1,5'-茚]-7a'(1'H)-基beta-D-吡喃葡萄糖苷


    CAS Name: 7'a-(b-D-Glucopyranosyloxy)-1',3'a,4',7'a-tetrahydro-4'-hydroxy-2',4',6'-trimethyl-(2'R,3'aR,4'S,7'aR)-spiro[cyclopropane-1,5'-[5H]inden]-3'(2'H)-one
    Additional Names: braxin C; PT Literature References: Norsequiterpene glucoside identified as the carcinogenic priniciple of the bracken ferns, Pteridium spp. Isoln from P. aquilinum var. latiusculum: H. Niwa et al., Tetrahedron Lett. 24, 4117 (1983). Structure elucidation: eidem, ibid. 5371. HPLC determn in ferns: M. P. Agnew, D. R. Lauren, J. Chromatogr. 538, 462 (1991). Mechanism of carcinogenesis: M. Ojika et al., Tetrahedron 43, 5261 (1987); A. S. Prakash et al., Nat. Toxins 4, 221 (1996). Levels in cow's milk and health implications: M. E. Alonso-Amelot et al., Lait 78, 413 (1998). Review of chemistry and carcinogenic mechanisms: K. Yamada et al., Angew. Chem. Int. Ed. 37, 1818-1826 (1998); of biological activity: M. Shahin et al., Mutat. Res. 443, 69-79 (1999).

  • Abrine CAS Registry Number: 526-31-8 相思豆毒素


    CAS Name: N-Methyl-L-tryptophan
    Additional Names: a-methylamino-b-(3-indole)propionic acid
    Percent Composition: C 66.04%, H 6.47%, N 12.84%, O 14.66%
    Literature References: Not to be confused with the albuminous substance abrin, q.v. Obtained from the seeds of Abrus precatorius L., Leguminosae (jequirity): Hoshino, Ann. 520, 31 (1935). Synthesis: Miller, Robson, J. Chem. Soc. 1938, 1910. Configuration: Cahill, Jackson, J. Biol. Chem. 126, 29 (1938).

  • Nomifensine CAS Registry Number: 24526-64-5 诺米芬辛


    CAS Name: 1,2,3,4-Tetrahydro-2-methyl-4-phenyl-8-isoquinolinamine
    Additional Names: 8-amino-1,2,3,4-tetrahydro-2-methyl-4-phenylisoquinoline
    Percent Composition: C 80.63%, H 7.61%, N 11.75%
    Literature References: Novel antidepressant distinguished from existing tricyclic and tetracyclic antidepressants by its bicyclic structure. Prepn: GB 1164192 corresp to G. Ehrhart et al., US 3577424 (1969, 1971, both to Farbwerke Hoechst); I. Hoffmann et al., Arzneim.-Forsch. 21, 1045 (1971). Pharmacology: I. Hoffmann, ibid. 23, 45 (1973); P. Hunt et al., J. Pharm. Pharmacol. 26, 370 (1974); B. Costall et al., Psychopharmacologia 41, 153 (1975). Pharmacokinetics: L. Vereczkey et al., ibid. 45, 225 (1975). Study on abuse potential in humans: C. Spyraki, H. C. Fibiger, Science 212, 1167 (1981). Review: Br. J. Clin. Pharmacol. 4, Suppl. 2 (1977) pp 1S-248S; Int. Pharmacopsychiatry 17, Suppl. 1 (1982) pp 1-148.

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