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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

  • Methyl Sulfide CAS Registry Number: 75-18-3 二甲基硫


    CAS Name: Thiobismethane
    Additional Names: dimethyl sulfide
    Percent Composition: C 38.66%, H 9.73%, S 51.61%
    Literature References: Metabolic product of many biosystems. Important flavor constituent in lager beer and in many cooked vegetables such as tomatoes and corn. Principal volatile sulfur compound in seawater; abundantly produced by marine algae. Prepn: V. Regnault, Ann. 34, 24 (1840); and properties: D. T. McAllan et al., J. Am. Chem. Soc. 73, 3627 (1951). Review of role in malting and brewing: C. J. Dickenson, Chem. Ind. 24, 896-898 (1979); B. J. Anness, C. W. Bamforth, J. Inst. Brew. 88, 244-252 (1982). Review of role in global sulfur cycle: P. S. Liss et al., Philos. Trans. R. Soc. London Ser. B 352, 159-169 (1997). Review of gas-phase chemistry: I. Barnes et al., Chem. Rev. 106, 940-975 (2006).

  • Palitantin CAS Registry Number: 15265-28-8


    CAS Name: (2R,3S,5R,6R)-rel-3-(1E,3E)-1,3-Heptadienyl-5,6-dihydroxy-2-(hydroxymethyl)cyclohexanone
    Percent Composition: C 66.12%, H 8.72%, O 25.16%
    Literature References: Metabolic product of Penicillium palitans Westling. Isoln: J. H. Birkinshaw, H. Raistrick, Biochem. J. 30, 801 (1936). Derivs and degradation products: J. H. Birkinshaw, ibid. 51, 271 (1952). Structure: K. Bowden et al., J. Chem. Soc. 1959, 1662. Biosynthesis: P. Chaplen, R. Thomas, Biochem. J. 77, 91 (1960); A. J. Birch, M. Kocor, J. Chem. Soc. 1960, 866. Reactivity studies: A. T. Austin, B. Pearson, Chem. Ind. (London) 1966, 1228. Stereoselective synthesis of (±)-form: A. Ichihara et al., Tetrahedron Lett. 1977, 3473; eidem, Tetrahedron 36, 1547 (1980).

  • Spinulosin CAS Registry Number: 85-23-4 棘青霉素


    CAS Name: 2,5-Dihydroxy-3-methoxy-6-methyl-2,5-cyclohexadiene-1,4-dione
    Additional Names: 2,5-dihydroxy-3-methoxy-6-methyl-p-benzoquinone; 3,6-dihydroxy-5-methoxy-p-toluquinone; 3,6-dihydroxy-4...
    Literature References: Metabolic product of the fungi Penicillium spinulosum Thom. and Aspergillus fumigatus Fres.: Birckinshaw, Raistrick, Philos. Trans. R. Soc. London B220, 245 (1931); Anslow, Raistrick, Biochem. J. 32, 2288 (1938); Pettersson, Acta Chem. Scand. 17, 1771 (1963). Structure: Aulin, Erdtman, Sven. Kem. Tidskr. 49, 208 (1937). Synthesis: Anslow, Raistrick, Biochem. J. 32, 803 (1938). Biosynthesis: Pettersson, Acta Chem. Scand. 19, 1016 (1965).

  • p-Anisaldehyde CAS Registry Number: 123-11-5 4-甲氧基苯甲醛; 对甲氧基苯甲醛; 大茴香醛


    CAS Name: 4-Methoxybenzaldehyde
    Additional Names: anisic aldehyde
    Percent Composition: C 70.57%, H 5.92%, O 23.50%
    Literature References: Metabolic product of the odoriferous fungus Lentinus lepidus Fr.: Birkinshaw et al., Biochem. J. 38, 131 (1944); of wood-rotting fungus Polyporus benzoinus (Wahl.) Fr.: Birkinshaw et al., ibid. 50, 509 (1952); of Daldalea juniperina Murr.: Birkinshaw, Chaplen, ibid. 60, 255 (1955). Prepn: Niedzielski, Nord, J. Am. Chem. Soc. 63, 1462 (1941); Sisti et al., J. Org. Chem. 27, 279 (1962). Toxicity study: P. M. Jenner et al., Food Cosmet. Toxicol. 2, 327 (1964).

  • Carglumic acid CAS Registry Number: 1188-38-1 N-氨基甲酰-L-谷氨酸


    CAS Name: N-(Aminocarbonyl)-L-glutamic acid
    Additional Names: carbamylglutamic acid; N-carbamoyl-L-glutamic acid; l-uramidoglutaric acid; ureidoglutaric acid
    Trademarks: Carbaglu (Orphan Eur...
    Literature References: Metabolically stable analog of N-acetylglutamate, a physiological activator of the first enzyme of the urea cycle, carbamylphosphate synthetase (CAPS). Prepn: H. McIlwain, Biochem. J. 33, 1942 (1939). Effect on blood urea and ammonia levels and potential clinical application: J.-E. O'Connor et al., Eur. J. Pediatr. 143, 196 (1985). Evaluation in treatment of CAPS deficiency: G. Kuchler et al., J. Inher. Metab. Dis. 19, 220 (1996); of N-acetylglutamate synthetase (NAGS) deficiency: B. Plecko et al., Eur. J. Pediatr. 157, 996 (1998).

  • Homovanillic Acid CAS Registry Number: 306-08-1 高香草酸


    CAS Name: 4-Hydroxy-3-methoxybenzeneacetic acid
    Additional Names: (4-hydroxy-3-methoxyphenyl)acetic acid; 4-hydroxy-3-methoxy-a-toluic acid
    Percent Composition: C 59.34%, H 5.53%, O 35.13%
    Literature References: Metabolite found in human urine. Prepn: F. Tiemann, N. Nagai, Ber. 10, 201 (1877); F. Mauthner, Ann. 370, 368 (1909); H. E. Fisher, H. Hibbert, J. Am. Chem. Soc. 69, 1208 (1947). End product of dopamine, q.v.: K. Shaw et al., J. Biol. Chem. 226, 255 (1957); M. Goodall, H. Alton, Biochem. Pharmacol. 25, 2635 (1968).

  • Opromazine CAS Registry Number: 969-99-3 氧氯丙嗪


    CAS Name: 2-Chloro-N,N-dimethyl-10H-phenothiazine-10-propanamine 5-oxide
    Additional Names: 2-chloro-10-[3-(dimethylamino)propyl]phenothiazine 5-oxide; 10-(g-dimethylaminopropyl)-3-chlorphenothi...
    Literature References: Metabolite of chlorpromazine, q.v.: Salzman, Brodie, J. Pharmacol. Exp. Ther. 118, 46 (1956). Preparation by enzymatic oxidation of chlorpromazine: Gillette, Kamm, ibid. 130, 262 (1960). Synthesis: FR 1167653 (1958 to Rhône-Poulenc). Toxicity data: Minami, Yoshimoto, Nara Igaku Zasshi 8, 50 (1957), C.A. 51, 16966a (1957).

  • Tofenacin CAS Registry Number: 15301-93-6 托芬那辛


    CAS Name: N-Methyl-2-[(2-methylphenyl)phenylmethoxy]ethanamine
    Additional Names: N-methyl-2-[(o-methyl-a-phenylbenzyl)oxy]ethylamine; N-demethylorphenadrine; N-methylaminoethyl 2-methylbenzhydr...
    Literature References: Metabolite of orphenadrine formed by N-demethylation. Prepn: BE 628167; Harms, US 3407258 (1963, 1968 both to Brocades-Stheeman Pharmacia). Resolution of isomers: van der Stelt et al., Arzneim.-Forsch. 19, 2010 (1969). Physical and chemical properties: Doorenbos et al., Pharm. Weekbl. 101, 525 (1966). Pharmacology: Funcke et al., Arch. Int. Pharmacodyn. 177, 28 (1969); Den Besten et al., Arzneim.-Forsch. 20, 538 (1970). Metabolic studies: Hespe, Prins, Eur. J. Pharmacol. 8, 119 (1969); Hespe, Kafoe, ibid. 13, 113 (1970). Clinical studies: Bram, Shanmuganathan, Curr. Ther. Res. 13, 625 (1971).

  • Acecainide CAS Registry Number: 32795-44-1 乙酰普卡胺


    CAS Name: 4-(Acetylamino)-N-[2-(diethylamino)ethyl]benzamide
    Additional Names: 4'-[[2-(diethylamino)ethyl]carbamoyl]acetanilide; N-acetylprocainamide; NAPA
    Percent Composition: C 64.96%, H 8...
    Literature References: Metabolite of procainamide, q.v. Prepn: E. C. Schreiber, DE 2062978 (1971 to Squibb), C.A. 75, 76427 (1972). Pharmacokinetics: M. Wierzchowiecki et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 18, 272 (1980). Clinical pharmacology and antiarrhythmic efficacy: J. Kluger et al., Am. J. Cardiol. 45, 1250 (1980); R. A. Winkle et al., ibid. 47, 123 (1981). HPLC determn in plasma: D. Raphanaud et al., Ther. Drug Monit. 8, 365 (1986). Review of pharmacology and therapeutic potential: D. W. G. Harron, R. N. Brogden, Drugs 39, 720-740 (1990).

  • Ponazuril CAS Registry Number: 69004-04-2 妥曲珠利砜


    CAS Name: 1-Methyl-3-[3-methyl-4-[4-[(trifluoromethyl)sulfonyl]phenoxy]phenyl]-1,3,5-triazine-2,4,6(1H,3H,5H)-trione
    Additional Names: toltrazuril sulfoneTrademarks: Marquis (Bayer)
    Percent ...
    Literature References: Metabolite of toltrazuril, q.v.; triazine trione antiprotozoal. Prepn: A. Haberkorn et al., DE 2718799; eidem, US 4219552 (1978, 1980 both to Bayer). Stereoselective generation by microsomes: E. Benoit et al., Biochem. Pharmacol. 46, 2337 (1993). LC/MS determn in meat and eggs: V. Hormazábal et al., J. Liq. Chromatogr. Relat. Technol. 26, 791 (2003). Activity vs Sarcocystis neurona, the causative agent of EPM: D. S. Lindsay et al., Vet. Parasitol. 92, 165 (2000); R. P. Franklin et al., ibid. 114, 123 (2003); vs Neospora canium: A. K. Darius et al., Parasitol. Res. 92, 453, 520 (2004).

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