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

LH-RH CAS Registry Number: 9034-40-6 戈那瑞林

CAS Name: Luteinizing hormone-releasing factor
Additional Names: LH-RF; luteinizing hormone-releasing hormone; LRF; LRH; gonadorelin; gonadotropin-releasing factor; gonadoliberin; luliberin; LH...
Literature References: Neurohumoral hormone produced in the hypothalamus which stimulates the secretion of the pituitary hormones, LH (luteinizing hormone) and FSH (follicle-stimulating hormone) q.q.v., which in turn produce changes resulting in the induction of ovulation. Isoln from porcine hypothalamic extracts: A. V. Schally et al., Biochem. Biophys. Res. Commun. 43, 393 (1971). Structure: Matsuo et al., ibid. 1334; Baba et al., ibid. 44, 459 (1971); Burgus et al., C.R. Seances Acad. Sci. Ser. D 273, 1611 (1971). Solid phase synthesis: Monahan et al., ibid. 508; Monahan, Rivier, Biochem. Biophys. Res. Commun. 48, 1100 (1972); Coy et al., Methods Enzymol. 37, 416 (1975); D. H. Rich, S. K. Gurwara, Tetrahedron Lett. 1975, 301. Industrial prepn: Geiger et al., DE 2213737 (1973 to Hoechst). Confirmation of biological activity: A. V. Schally et al., Science 173, 1036 (1971). Pharmacokinetics: T. W. Redding, J. Clin. Endocrinol. Metab. 37, 626 (1973). Reviews of physiology and implications in fertility control: A. V. Schally et al., Fertil. Steril. 22, 703 (1971); R. Guillemin, Contraception 6, 1 (1972). Review of LH-RH and other hypothalamic hormones: A. V. Schally et al., Science 179, 341 (1973); A. V. Schally, ibid. 202, 18-28 (1978); of LH-RH and somatostatin, q.v.: S. M. McCann, Annu. Rev. Pharmacol. Toxicol. 22, 491-515 (1982). General reviews: J. Sandow, Clin. Endocrinol. 18, 571-592 (1983); S. M. McCann, J. Endocrinol. Invest. 6, 243-251 (1983).

Murexine CAS Registry Number: 20284-40-6

CAS Name: 2-[[3-(1H-Imidazol-4-yl)-1-oxo-2-propenyl]oxy]-N,N,N-trimethylethanaminium
Additional Names: b-(4-imidazolyl)acrylcholine; urocanylcholine
Literature References: Neuromuscular blocker found, often in very large quantities, in the median zone of the hypobranchial body of Murex trunculus and of other related species of mollusks: Erspamer, Dordoni, Ric. Sci. Ricostr. 16, 1114 (1946); Arch. Int. Pharmacodyn. 74, 263 (1947); Erspamer, ibid. 76, 308 (1948). Isoln: idem, Experientia 4, 226 (1948); M. Roseghini et al., Eur. J. Biochem. 12, 468 (1970); J. E. Blankenship et al., Comp. Biochem. Physiol. 51C, 129 (1975). Synthesis: Pasini et al., Ann. 578, 6 (1952); Pasini, Coda, US 2956061 (1960 to Società Farmaceutici). Structure: V. Erspamer, O. Benati, Science 117, 161 (1953). Effect on vertebrate and invertebrate muscles: J. C. de Freitas, Comp. Biochem. Physiol. 56C, 57 (1977).

Hexafluorenium Bromide CAS Registry Number: 317-52-2 己芴溴铵

CAS Name: N,N'-Di-9H-fluoren-9-yl-N,N,N',N'-tetramethyl-1,6-hexanediaminium dibromide
Additional Names: hexamethylenebis[9-fluorenyldimethylammonium bromide]; hexamethylenebis(dimethyl-9-fluore...
Literature References: Neuromuscular blocking agent with pseudocholinesterase inhibitory activity. Prepn: Cavallito et al., J. Am. Chem. Soc. 76, 1862 (1954); Cavallito, Gray, US 2783237 (1957 to Irwin, Neisler). Clinical trial for prolongation of succinylcholine muscular block: L. F. Walts et al., Anesthesiology 33, 503 (1970). Review: R. M. Britton, M. Figueroa, Anesth. Analg. 52, 100-105 (1973).

Kalkitoxin CAS Registry Number: 247184-89-0

CAS Name: (2R)-N-[(3S,5S,6R)-7-[(4R)-4-Ethenyl-4,5-dihydro-2-thiazolyl]-3,5,6-trimethylheptyl]-N,2-dimethylbutanamide
Percent Composition: C 68.80%, H 10.45%, N 7.64%, O 4.36%, S 8.75%
Literature References: Neurotoxic lipopeptide isolated from the Caribbean marine algae, Lyngbya majuscula. Isoln, structure determn and synthesis: M. Wu et al., J. Am. Chem. Soc. 122, 12041 (2000). NMDA-receptor based neurotoxicity: F. W. Berman et al., Toxicon 37, 1645 (1999). Total synthesis: T. Asano et al., Tennen Yuki Kagobutsu Toronkai Koen Yoshishu 2000, 691. Brief review: J. Fricker, Drug Devel. Today 6, 223-224 (2001).

Apamin CAS Registry Number: 24345-16-2 蜂毒明肽

Percent Composition: C 46.80%, H 6.51%, N 21.42%, O 18.94%, S 6.33%
Literature References: Neurotoxic polypeptide consisting of 18 amino acid residues and 2 disulfide bridges. Comprises about 2% by wt of the dried venom of Apis mellifica (mellifera), the honey bee. Isoln: E. Habermann, K. G. Reiz, Naturwissenschaften 51, 61 (1964); eidem, Biochem. Z. 341, 451 (1965). Structure: P. Haux et al., Z. Physiol. Chem. 348, 737 (1967); R. Shipolini et al., Chem. Commun. 1967, 679. Conformation: R. C. Hider, U. Ragnarsson, FEBS Lett. 111, 189 (1980); B. Busetta, ibid. 112, 138 (1980). Solution structure: J. H. B. Pease, D. E. Wemmer, Biochemistry 27, 8491 (1988). Solid-phase synthesis: J. van Rietschoten et al., Eur. J. Biochem. 56, 35 (1975); B. E. B. Sandberg, U. Ragnarsson, Int. J. Pept. Protein Res. 11, 238 (1978). Pharmacology: Wellheoner, Arch. Pharmakol. Exp. Pathol. 262, 29 (1969). Biochemistry: E. Habermann, K. G. Reiz, Biochem. Z. 343, 192 (1965). Action on CNS: E. Habermann, D. Cheng-Raude, Toxicon 13, 465 (1975). Binding and toxicity studies: C. Labbé-Jullié et al., Eur. J. Biochem. 196, 639 (1991). Review: E. Habermann, Science 177, 314-322 (1972); C. Granier, J. van Rietschoten, in Natural Toxins, D. Eaker, T. Wadström, Eds. (Pergamon, New York, 1980) pp 481-486; E. Habermann, Pharmacol. Ther. 25, 255-270 (1984).

Isaxonine CAS Registry Number: 4214-72-6 伊沙索宁

CAS Name: N-(1-Methylethyl)-2-pyrimidinamine
Additional Names: 2-(isopropylamino)pyrimidine
Percent Composition: C 61.29%, H 8.08%, N 30.63%
Literature References: Neurotropic agent that promotes neurite outgrowth. Prepn: D. J. Brown, J. S. Harper, J. Chem. Soc. 1965, 5542. Prepn of pharmacologically active salts: A. Esanu, BE 788648; idem, US 3984414; idem, DE 2707095; idem, US 4073895 (1973, 1976, 1977, 1978 all to Soc. d'Etudes Prod. Chim.). Nerve growth promoting action: A. Hugelin et al., C.R. Seances Acad. Sci. Ser. D 285, 1339 (1977); eidem, Experientia 35, 626 (1979). Enhancement of muscle re-innervation in man: A. Sebille, A. Hugelin, Br. J. Pharmacol. 9, 275 (1980). Series of articles on in vitro effects, pharmacology, clinical studies: Nouv. Presse Med. 11, 1189-1280 (1982).

Sivelestat CAS Registry Number: 127373-66-4 西维来司他

CAS Name: N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]glycine
Additional Names: N-[o-(p-pivaloyloxybenzene)sulfonylaminobenzoyl]glycine; N-[2-[4-(2,2-dimethylpropionyloxy...
Literature References: Neutrophil elastase inhibitor. Prepn: K. Imaki et al., EP 347168; eidem, US 5017610 (1989, 1991 both to Ono); and structure-activity study: K. Imaki et al., Bioorg. Med. Chem. 4, 2115 (1996). Pharmacology: K. Kawabata et al., Biochem. Biophys. Res. Commun. 177, 814 (1991). HPLC determn in plasma and urine: T. Shintani et al., J. Pharm. Biomed. Anal. 12, 397 (1994). Pharmacokinetics and metabolism in rats: F. Watanabe et al., Biol. Pharm. Bull. 20, 392 (1997). Enzyme inhibition in ex vivo human pleural effusion: T. Sakuma et al., Eur. J. Pharmacol. 353, 273 (1998). Acute toxicity: H. Yanagi et al., J. Toxicol. Sci. 23, Suppl. 3, 409 (1998), C.A. 130, 20355 (1998). Review: L. Pradella, Curr. Opin. Anti-Inflam. Immunomod. Invest. Drugs1, 485-501 (1999).

Cephaeline CAS Registry Number: 483-17-0 吐根酚碱

CAS Name: 7',10,11-Trimethoxyemetan-6'-ol
Additional Names: desmethylemetine; dihydropsychotrine
Percent Composition: C 72.07%, H 8.21%, N 6.00%, O 13.72%
Literature References: Next to emetine the most important alkaloid of ipecac, the ground roots of Uragoga ipecacuanha (Brot.) Baill. [Cephaelis ipecacuanha (Brot.) A. Rich.], Rubiaceae: Carr, Pyman, J. Chem. Soc. 105, 1591 (1914); Hesse, Ann. 405, 1 (1914). Structure: Pailer, Porschinski, Monatsh. Chem. 80, 101 (1949). Stereochemistry: Van Tamelen et al., J. Am. Chem. Soc. 79, 4817 (1957). Partial synthesis: A. K. Garg, J. R. Gear, Tetrahedron Lett. 50, 4377 (1969). Biosynthetic studies: eidem, ibid. 1968, 141. HPLC determn in biological fluids: D. J. Crouch et al., J. Anal. Toxicol. 8, 63 (1984). Review: M. Janot in Manske, Holmes, The Alkaloids vol. 3 (Academic Press, New York, 1953) pp 363-394.

Nicorandil CAS Registry Number: 65141-46-0 尼可地尔

CAS Name: N-[2-(Nitrooxy)ethyl]-3-pyridinecarboxamide
Additional Names: N-(2-hydroxyethyl)nicotinamide nitrate (ester)Trademarks: Adancor (Merck-Cl'enot); Ikorel (RPR); Perisalol (Chugai); Sigm...
Literature References: Nicotinamide derivative; exhibits dual mechanism of action as both nitrovasodilator and potassium channel activator. Prepn: H. Nagano et al., DE 2714713; eidem, US 4200640 (1977, 1980 both to Chugai). Pharmacology: N. Taira et al., Clin. Exp. Pharmacol. Physiol. 6, 301 (1979). Mechanism of action: F. Yoneyama et al., Cardiovasc. Drugs Ther. 4, 1119 (1990). Symposia on pharmacology and clinical efficacy: Am. J. Cardiol. 63, Suppl, 1J-85J (1989); J. Cardiovasc. Pharmacol. 20, Suppl. 3, S1-S108 (1992). Review of clinical potential in ischemic heart disease: H. Purcell, K. Fox, Br. J. Clin. Pract. 47, 150-154 (1993). Clinical prevention of coronary events in patients with angina: IONA Study Group, Lancet 359, 1269 (2002).

Cotinine CAS Registry Number: 486-56-6 吡啶吡咯酮

CAS Name: 1-Methyl-5-(3-pyridinyl)-2-pyrrolidinone
Additional Names: N-methyl-2-(3-pyridyl)-5-pyrrolidone
Percent Composition: C 68.16%, H 6.86%, N 15.90%, O 9.08%
Literature References: Nicotine metabolite first described by Pinner, Arch. Pharm. 231, 378 (1893). Isolated from autoxidized nicotine, nicotine treated with hydrogen peroxide, from nicotine irradiated with ultraviolet light: Frankenburg, Vaitekunas, J. Am. Chem. Soc. 79, 149 (1957).