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

Aclatonium Napadisilate CAS Registry Number: 55077-30-0 萘二磺酸乙乳胆铵

CAS Name: 2-[2-(Acetyloxy)-1-oxopropoxy]-N,N,N-trimethylethanaminium 1,5-naphthalenedisulfonate (2:1)
Additional Names: 1,5-naphthalenedisulfonic acid bis [2-[2-(acetyloxy)-1-oxopropoxy]-N,N,N-...
Literature References: Spasmolytic agent related structurally to acetylcholine chloride, q.v. Prepn: K. Miura et al., DE 2425983; eidem, US 3903137 (1973, 1975 both to Toyama). Synthesis and smooth muscle activity: eidem, Yakugaku Zasshi 99, 1245 (1979), C.A. 92, 146197r (1980). Toxicity study: A. Takai et al., Oyo Yakuri 19, 93 (1980), C.A. 93, 613367 (1980). Series of articles on metabolism, pharmacology, toxicity studies: Oyo Yakuri 18, 695-942 (1979), C.A. 92, 191015r, 191281z, 191282a, 208995k-7n (1980).

Eperisone CAS Registry Number: 64840-90-0 乙哌立松

CAS Name: 1-(4-Ethylphenyl)-2-methyl-3-(1-piperidinyl)-1-propanone
Additional Names: 4'-ethyl-2-methyl-3-piperidinopropiophenone
Percent Composition: C 78.72%, H 9.71%, N 5.40%, O 6.17%
Literature References: Spasmolytic agent related structurally to tolperisone, q.v. Prepn: E. Morita et al., DE 2458638; E. Morita, T. Kanai, US 4181803 (1975, 1980 both to Eisai). Pharmacological study: K. Tanaka et al., Nippon Yakurigaku Zasshi 77, 511 (1981), C.A. 95, 35471t (1981). Absorption, distribution, excretion in rats and guinea pigs: T. Fujita et al., Oyo Yakuri 21, 835 (1981), C.A. 96, 28193w (1982). Toxicity study: H. Miyagawa et al., ibid. 939, C.A. 96, 79722a (1982).

Cimetropium Bromide CAS Registry Number: 51598-60-8 西托溴铵

CAS Name: (1a,2b,4b,5a,7b)-9-(Cyclopropylmethyl)-7-[(2S)-3-hydroxy-1-oxo-2-phenylpropoxy]-9-methyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide
Additional Names: 8-(cyclopropylmethyl)-6b,7b...
Literature References: Spasmolytic agent with affinity for intestinal muscarinic receptors. Prepn: S. Casadio, A. Donetti, DE 2316728; eidem, US 3853886 (1973, 1974 both to De Angeli). Crystal and molecular structure: G. Giuseppetti et al., Farmaco Ed. Sci. 35, 231 (1980). Molecular conformation in solution: A. Gallazzi et al., ibid. 913. Pharmacology: A. Schiavone et al., Arzneim.-Forsch. 35, 796 (1985); C. Scarpignato, G. Bianchi Porro, Int. J. Clin. Pharmacol. Res. 5, 467 (1985). Clinical trials in treatment of irritable bowel syndrome: G. Piai et al., Clin. Trials J. 23, 6 (1986); A. Ferrari et al., Clin. Ther. 8, 320 (1986).

Rociverine CAS Registry Number: 53716-44-2 罗西维林

CAS Name: 1-Hydroxy[1,1'-bicyclohexyl]-2-carboxylic acid 2-(diethylamino)-1-methylethyl ester
Additional Names: 2-(diethylamino)-1-methylethyl cis-1-hydroxy[bicyclohexyl]-2-carboxylateTrademark...
Literature References: Spasmolytic agent with balanced neurotropic and myotropic properties. Prepn: L. Turbanti, ZA 6705649 C.A. 70, 47117d (1969) and US 3700675 (1968, 1972 both to Guidotti). Antispasmodic activity in vitro and in vivo: G. Toson et al., Arzneim.-Forsch. 28, 1130 (1978). Effect in cystitis or bladder spasm: A. Manganelli, Farmaco Ed. Prat. 34, 384 (1979). Clinical studies: M. Petrillo et al., Curr. Med. Res. Opin. 7, 73 (1980); R. Assisi, S. deStefano, Acta Ther. 6, 353 (1980); F. Marsala, Minerva Med. 73, 2179 (1982).

Pinaverium Bromide CAS Registry Number: 53251-94-8 匹维溴铵

CAS Name: 4-[(2-Bromo-4,5-dimethoxyphenyl)methyl]-4-[2-[2-(6,6-dimethylbicyclo[3.1.1]hept-2-yl)ethoxy]ethyl]morpholinium bromide
Additional Names: 4-(6-bromoveratryl)-4-[2-[2-(6,6-dimethyl-2-no...
Literature References: Spasmolytic agent with low incidence of anticholinergic effects. Prepn: BE 769469; R. Baronnet, US 3845048 (1971, 1974 both to Societe Berri-Balzac). Synthesis and pharmacology: R. Baronnet et al., Eur. J. Med. Chem. 9, 182 (1974). Pharmacodynamics: J. Bretaudeau et al., Therapie 30, 919 (1975). Synthesis of 14C pinaverium bromide and pharmacokinetics: C. Jacquot et al., Eur. J. Med. Chem. 13, 61 (1978). Mechanism of action: J. Bretaudeau, O. Foussard-Blanpin, J. Pharmacol. 11, 233 (1980). Inhibition of gastrointestinal contractile activity in dogs: Z. Itoh, T. Takahashi, Arzneim.-Forsch. 31, 1450 (1981). Effects in humans on gastric emptying and transit time: J. Bertrand et al., Therapie 36, 555 (1981).

Visnagin CAS Registry Number: 82-57-5 齿阿米素; 甲氧呋豆素

CAS Name: 4-Methoxy-7-methyl-5H-furo[3,2-g][1]benzopyran-5-one
Additional Names: 5-methoxy-2-methylfuranochromone
Percent Composition: C 67.82%, H 4.38%, O 27.80%
Literature References: Spasmolytic constituent of Ammi visnaga Lam., Umbelliferae. One of the active principles in the Egyptian traditional medicine known as "khella" that is used as a diuretic and vasodilator. See also: visnadine, khellin. Isoln and structure: Späth, Gruber, Ber. 74, 1492 (1941). Synthesis: Aneja et al., Tetrahedron 3, 230 (1958); Badawi, Fayez, Tetrahedron Lett. 1967, 1029. HPLC determn in A. visnaga fruit: M. M. El-Domiaty, J. Pharm. Sci. 81, 475 (1992).

Somatotropin CAS Registry Number: 9002-72-6 生长激素

Additional Names: Adenohypophyseal growth hormone; GH; hypophyseal growth hormone; anterior pituitary growth hormone; growth hormone; phyone; pituitary growth hormone; somatotropic hormone; STH
Literature References: Species-specific anabolic protein that promotes somatic growth, stimulates protein synthesis, and regulates carbohydrate and lipid metabolism. Increases serum levels of somatomedins, q.v. Secreted by the anterior pituitary under the regulation of the hypothalamic hormones, somatoliberin and somatostatin, q.q.v. Growth hormones from various species differ in amino acid sequence, antigenicity, isoelectric point, and in the range of animals in which they can produce biological responses. Isoln from bovine anterior pituitary substance: C. H. Li et al., J. Biol. Chem. 159, 353 (1945); A. E. Wilhelmi et al., ibid. 176, 735 (1948); C. H. Li, US 3118815 (1964 to Upjohn). Isoln from human pituitaries: Lewis, Brink, US 2974088 (1961 to Merck Co.); Reisfeld et al., Endocrinology 71, 559 (1962). Amino acid sequence of human growth hormone (HGH): C. H. Li et al., J. Am. Chem. Soc. 88, 2050 (1966); eidem, Arch. Biochem. Biophys. 133, 70 (1969). Total synthesis: C. H. Li, D. Yamashiro, J. Am. Chem. Soc. 92, 7608 (1970). Revised sequence of HGH: H. D. Niall, Nature New Biol. 230, 90 (1971). Review of structural studies and comparison with the lactogenic hormones: H. D. Niall et al., Recent Prog. Horm. Res. 29, 387-416 (1973). Review of protein chemistry: C. H. Li, Mol. Cell. Biochem. 46, 31-41 (1982). Cloning and expression of cDNA for HGH in E. coli: D. V. Goeddel et al., Nature 281, 544 (1979); D. V. Goeddel, H. L. Heyneker, BE 884012; eidem, US 4342832 (1980, 1982 both to Genentech); in mammalian cells: G. N. Pavakis et al., Proc. Natl. Acad. Sci. USA 78, 7398 (1981). Purification and bioactivity of recombinant HGH: K. C. Olson et al., Nature 293, 408 (1981). Clinical comparison of natural and recombinant HGH: R. L. Hintz et al., Lancet 1, 1276 (1982). Use of recombinant bovine GH to increase milk production in cows: D. E. Bauman et al., J. Dairy Sci. 68, 1352 (1985). Discussion of use of recombinant GH in applied animal agriculture: J. L. Burton, B. W. McBride, J. Agric. Ethics 2, 129-159 (1989). Review of GH gene studies: D. D. Moore et al., Recent Prog. Horm. Res. 38, 197-225 (1982). Review of bioregulation of HGH secretion: D. G. Johnston et al., J. R. Soc. Med. 78, 319-327 (1985); of mechanism of action on target cells: O. G. P. Isaksson et al., Annu. Rev. Physiol. 47, 483-499 (1985). Symposium on pharmacology and clinical efficacy: Horm. Res. 33, Suppl. 4, 1-107 (1990). Books: Growth and Growth Hormone, A. Pecile, E. Muller, Eds. (Excerpta Medica, Amsterdam, 1972); Human Growth Hormone and Gonadotrophins in Health and Disease, P. Franchimont, H. Burger, Eds. (Elsevier, New York, 1975) 494 pp; Growth Hormone and Other Biologically Active Peptides, A. Pecile, E. Muller, Eds. (Elsevier, New York, 1980); Evaluation of Growth Hormone Secretion, Z. Laron, O. Butenandt, Eds. (S. Karger, New York, 1983); Use of Somatotropin in Livestock Production, K. Sejrsen et al., Eds. (Elsevier, New York, 1989).

Tamsulosin CAS Registry Number: 106133-20-4 坦索洛新

CAS Name: 5-[(2R)-2-[[2-(2-Ethoxyphenoxy)ethyl]amino]propyl]-2-methoxybenzenesulfonamide
Additional Names: amsulosin
Percent Composition: C 58.80%, H 6.91%, N 6.86%, O 19.58%, S 7.85%
Literature References: Specific a1-adrenoceptor antagonist. Prepn: K. Imai et al., EP 34432; eidem, US 4703063 (1981, 1987 both to Yamanouchi). Comparative pharmacology of enantiomers and racemate: K. Honda et al., Arch. Pharmacol. 336, 295 (1987). HPLC determn in plasma: Y. Soeishi et al., J. Chromatogr. 533, 291 (1990). Clinical trials in benign prostatic hypertrophy: K. Kawabe et al., J. Urol. 144, 908 (1990); P. Abrams et al., Br. J. Urol. 76, 325 (1995). Review of pharmacology and clinical experience in urological disorders: M. C. Michel, J. J. de la Rosette, Expert Opin. Pharmacother. 5, 151-160 (2004).

Atipamezole CAS Registry Number: 104054-27-5 阿替美唑

CAS Name: 4-(2-Ethyl-2,3-dihydro-1H-inden-2-yl)-1H-imidazole
Additional Names: 4(5)-(2-ethyl-2-indanyl)imidazole
Percent Composition: C 79.21%, H 7.60%, N 13.20%
Literature References: Specific a2-adrenoceptor antagonist. Prepn: A. J. Karjalainen et al., EP 183492; eidem, US 4689339 (1986, 1987 both to Farmos). Behavioral and neurochemical effects: H. Scheinin et al., Eur. J. Pharmacol. 151, 35 (1988). Pharmacodynamics and pharmacokinetics: X. Fargetton, T. Vähä-Vahe, Tijdschr. Diergeneeskd 114, Suppl. 1, 91S (1989). Binding study in comparison with yohimbine, q.v.: R. Virtanen et al., Arch. Int. Pharmacodyn. 297, 190 (1989). Attenuation of ethanol effects in mice: M. J. Durcan et al., Alcohol 6, 189 (1989). Preliminary report as detomidine, q.v., antagonist in horses: L. Nilsfors, C. Kvart, Acta Vet. Scand. 82, 121 (1986). Use as medetomidine, q.v., antagonist in zoo animals: H. Jalanka, ibid. 85, 193 (1989).

Ispronicline CAS Registry Number: 252870-53-4 异丙克兰

CAS Name: (2S,4E)-N-Methyl-5-[5-(1-methylethoxy)-3-pyridinyl]-4-penten-2-aminePercent Composition: C 71.75%, H 9.46%, N 11.95%, O 6.83%
Literature References: Specific a4b2 nicotinic receptor agonist. Prepn: W. S. Caldwell et al., WO 9965876 (1999 to R. J. Reynolds); eidem, US 6958399 (2005 to Targacept). Effect on cortical acetylcholine release in rats: M. C. Obinu et al., Prog. Neuro-Psychopharmacol. Biol. Psychiatry 26, 913 (2002). Review of pharmacology: G. J. Gatto et al., CNS Drug Rev. 10, 147-166 (2004); and clinical experience: H. Geerts, Curr. Opin. Invest. Drugs 7, 60-69 (2006).