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

Epostane CAS Registry Number: 80471-63-2 环氧司坦

CAS Name: (4a,5a,17b)-4,5-Epoxy-3,17-dihydroxy-4,17-dimethylandrost-2-ene-2-carbonitrile
Additional Names: (2a,4a,5a,17b)-4,5-epoxy-17-hydroxy-4,17-dimethyl-3-oxoandrostane-2-carbonitrilePercen...
Literature References: 3b-Hydroxysteroid dehydrogenase inhibitor; derivative of trilostane, q.v. Prepn as ketone tautomer: R. G. Christiansen, DE 2855091; idem, US 4160027 (both 1979 to Sterling). Pharmacology and interceptive activity: J. E. Creange et al., Contraception 24, 289 (1981); R. G. Christiansen et al., J. Med. Chem. 27, 928 (1984). Clinical pharmacology: Z. M. Van der Spuy et al., Clin. Endocrinol. 19, 521 (1983); N. S. Pattison et al., Fertil. Steril. 42, 875 (1984). Clinical evaluation as abortifacient: L. Birgerson et al., Contraception 35, 111 (1987); M. J. Crooij et al., N. Engl. J. Med. 319, 813 (1988). Comparative clinical study with mifepristone, q.v., as abortifacient: L. Birgerson, V. Odlind, Fertil. Steril. 48, 565 (1987). Induction of labor in swine: P. A. Martin et al., J. Anim. Sci. 64, 497 (1987); in sheep: M. Silver, Vet. Rec. 120, 299 (1987). Regulation of ovulation in sheep: R. Webb, J. Reprod. Fertil. 79, 231 (1987). Abortifacient efficacy in dogs: D. M. Keister et al., Theriogenology 30, 497 (1988).

Durapatite CAS Registry Number: 1306-06-5 羟基磷灰石

CAS Name: Hydroxylapatite
Additional Names: calcium phosphate hydroxide; calcium orthophosphate basic; hydroxyapatite
Trademarks: Alveograf; Ossopan; Periograf
Literature References: 3Ca3(PO4)2.Ca(OH)2 or Ca10(PO4)6(OH)2. Also considered as pentacalcium monohydroxyorthophosphate Ca5(OH)(PO4)3. Calcd as Ca10H2O26P6; Ca 39.89%, H 0.20%, O 41.41%, P 18.50%. Occurs as a mineral in phosphate rock. Constitutes the mineral portion of bone. Prepn from Ca(NO3)2 and KH2PO4: Warington, J. Chem. Soc. 26, 983 (1873); Rathje, Ber. 74, 342 (1941); Hayek in Handbook of Preparative Inorganic Chemistry, G. Brauer, Ed. (Academic Press, 2nd ed., 1963) p 545; from calcium phosphate, dibasic: Perloff, Posner, Inorg. Synth. 6, 16 (1960); from Ca(NO3)2.4H2O and (NH4)3PO4 plus NH4OH: Hayek, Newesely, ibid. 7, 63 (1963). Formation and structure of synthetic bone hydroxyapatites: A. S. Posner et al., Prog. Cryst. Growth Charact. 3, 3 (1980).

Epristeride CAS Registry Number: 119169-78-7 爱普列特

CAS Name: (17b)-17-[[(1,1-Dimethylethyl)amino]carbonyl]androsta-3,5-diene-3-carboxylic acid
Additional Names: 17b-(N-tert-butylcarboxamido)androsta-3,5-diene-3-carboxylic acidPercent Compositio...
Literature References: 5a-Reductase inhibitor. Prepn and in vitro activity: D. A. Holt et al., EP 289327; eidem, US 4910226 and US 5017568 (1988, 1990, 1991 all to SmithKline Beecham); D. A. Holt et al., J. Med. Chem. 33, 943 (1990). Pharmacology: J. C. Lamb et al., Endocrinology 130, 685 (1992). Antitumor effects in rats: J. C. Lamb et al., Prostate 21, 15 (1992). Mechanism of action study: M. A. Levy et al., Biochemistry 29, 2815 (1990). HPLC determn in human plasma: V. K. Boppana et al., J. Chromatogr. 631, 251 (1993).

Sitamaquine CAS Registry Number: 57695-04-2 西罗莫斯

CAS Name: N,N-Diethyl-N'-(6-methoxy-4-methyl-8-quinolinyl)-1,6-hexanediamine
Additional Names: 8-(6'-diethylaminohexylamino)-6-methoxylepidine; 6-methoxy-8-(6-diethylaminohexylamine)-4-methylqu...
Literature References: 8-Aminoquinolone; analog of the antimalarial agent primaquine, q.v. Prepn: K. N. Campbell et al., J. Am. Chem. Soc. 68, 1556 (1946); idem, US 2508937 (1950 to USA, as represented by the Secy. of War). Antileishmanial activity in hamsters: K. E. Kinnamon et al., Am. J. Trop. Med. Hyg. 27, 751 (1978). HPLC determn in plasma: J. C. Anders et al., J. Chromatogr. 311, 117 (1984). Clinical evaluation in AIDS-associated Pneumocystis carinii pneumonia: B. G. Petty et al., J. Acquir. Immune Defic. Syndr. 21, 26 (1999); in visceral leishmaniasis: R. Dietze et al., Am. J. Trop. Med. Hyg. 65, 685 (2001). Ex vivo use in prevention of transfusion-associated Chagas' disease: H. Moraes-Souza et al., Rev. Soc. Bras. Med. Trop. 35, 563 (2002). Review of clinical development: C. Yeates, Curr. Opin. Invest. Drugs 3, 1446-1452 (2002); H. Sangraula et al., J. Assoc. Physicians India 51, 686-690 (2003).

Prenalterol CAS Registry Number: 57526-81-5 普瑞特罗

CAS Name: 4-[(2S)-2-Hydroxy-3-[(1-methylethyl)amino]propoxy]phenol
Additional Names: (-)-(S)-1-(p-hydroxyphenoxy)-3-(isopropylamino)-2-propanol
Percent Composition: C 63.98%, H 8.50%, N 6.22...
Literature References: A b1-adrenergic agonist. Prepn: K. A. Jaeggi et al., DE 2503968 corresp to US 3978041 and US 4049797 (1974, 1976, 1977, all to Ciba-Geigy). Pharmacologic study: E. Carlsson et al., Arch. Pharmacol. 300, 101 (1977). Metabolism, hemodynamic effects, pharmacokinetics in man: O. Rönn et al., Eur. J. Clin. Pharmacol. 17, 81 (1980). Cardiovascular effects: D. H. Scott et al., Br. J. Clin. Pharmacol. 7, 365 (1979). Clinical study in coronary heart disease: I. Hutton et al., Br. Heart J. 43, 134 (1980). See also T. P. Kenakin, D. Beek, J. Pharmacol. Exp. Ther. 213, 406 (1980) for a discussion of the selectivity of action. Prepns of the racemic mixture: NL 6409883 corresp to H. Köppe et al., US 3637852 (1965, 1972 both to Boehringer, Ing.); NL 301580 corresp to A. F. Crowther, L. H. Smith, US 3501769 (1965, 1970 both to ICI); A. F. Crowther et al., J. Med. Chem. 12, 638 (1969). Symposium: Acta Med. Scand. Suppl. 659, 1-325 (1982).

Carbuterol CAS Registry Number: 34866-47-2 卡布特罗

CAS Name: [5-[2-[(1,1-Dimethylethyl)amino]-1-hydroxyethyl]-2-hydroxyphenyl]urea
Additional Names: a-(t-butylaminomethyl)-4-hydroxy-3-ureidobenzyl alcohol
Percent Composition: C 58.41%, H 7.9...
Literature References: A b-adrenergic agonist related to isoproterenol, q.v., with selectivity for airway smooth muscle receptors. Prepn: C. Kaiser, S. T. Ross, DE 2106620; eidem, US 3763232 (1971, 1973 both to SKF); C. Kaiser et al., J. Med. Chem. 17, 49 (1974). Pharmacology, mechanism of action, toxicity study: J. R. Wardell et al., J. Pharmacol. Exp. Ther. 189, 167 (1974). Analysis in aq soln: L. J. Ravin et al., J. Pharm. Sci. 67, 1523 (1978). Clinical study: T. D. James, H. A. Lyons, J. Am. Med. Assoc. 241, 704 (1979).

Tulobuterol CAS Registry Number: 41570-61-0 妥布特罗

CAS Name: 2-Chloro-a-[[(1,1-dimethylethyl)amino]methyl]benzenemethanol
Additional Names: a-[(tert-butylamino)methyl]-o-chlorobenzyl alcohol
Percent Composition: C 63.29%, H 7.97%, Cl 15.57%,...
Literature References: A b-adrenergic receptor agonist, related structurally to terbutaline, q.v. Prepn: H. Kato, S. Kurata, DE 2244737 (1973 to Hokuriku), C.A. 78, 147538a (1973). Pharmacology: S. Kubo et al., Arzneim.-Forsch. 25, 1028 (1975); eidem, ibid. 27, 1433 (1977); I. Uesaka et al., ibid. 1439. Metabolism: T. Fujiihashi et al., Oyo Yakuri 18, 347 (1979), C.A. 92, 121781 (1980); K. Matsumura et al., Yakugaku Zasshi 101, 198 (1981), C.A. 94, 167404 (1981). Determn of tulobuterol and its metabolites in human urine: eidem, J. Chromatogr. 222, 53 (1981). Toxicological studies: S. Kubo et al., Oyo Yakuri 13, 197, 317 (1977), C.A. 88, 83591-2 (1978).

Colestipol CAS Registry Number: 26658-42-4 考来替泊

CAS Name: N-(2-Aminoethyl)-N'-[2-[(2-aminoethyl)amino]ethyl]-1,2-ethanediamine polymer with (chloromethyl)oxirane
Literature References: A basic anion exchange resin described as a high molecular wt copolymer of diethylenetriamine and 1-chloro-2,3-epoxypropane (hydrochloride), with approx 1 out of 5 amine nitrogens protonated, for which no structural formula has been assigned and for which no specific mol wt information is available, due to the highly cross-linked and insoluble nature of the material. Prepn: Nelson, Van den Berg, DE 1927336; eidem, US 3692895 (1969, 1971 to Upjohn); Lednicer, Peery, DE 2053585; eidem, US 3803237 (1971, 1974 to Upjohn). Activity studies: Parkinson et al., Atherosclerosis 11, 531 (1970); 17, 167 (1973); Marmo et al., G. Arterioscler. 8, 229 (1970); Goodman et al., J. Clin. Invest. 52, 2646 (1973). Toxicology: Webster, Bollert, Toxicol. Appl. Pharmacol. 28, 57 (1974). Review of pharmacology and therapeutic efficacy: R. C. Heel et al., Drugs 19, 161-180 (1980).

Bismuth Subnitrate CAS Registry Number: 1304-85-4 次硝酸铋

CAS Name: Bismuth hydroxide nitrate oxide (Bi5(OH)9(NO3)4O)
Additional Names: bismuth nitrate basic; bismuth oxynitrate; bismuth subnitricum; bismuthyl nitrate; bismuth white; magistery of bism...
Literature References: A basic salt, the compn of which varies with the conditions of preparation. Contains 70 to 74% Bi or 79 to 82% Bi2O3. Prepd by partial hydrolysis of Bi(NO3)3: Gmelins, Bismuth (8th ed.) 19, pp 132-135 (1927); Traité Pharm. Chim. vol. 1, P. Lebeau, M. M. Janot, Eds. (Masson, Paris, 1956) p 371; Handbuch der Pharmazie vol. 4(1), H. Thoms, Ed. (Urban Schwarzenberg, Berlin, 1927) p 325. Mechanism of action study: S. Pugh, M. R. Lewin, J. Gastroenterol. Hepatol. 5, 382 (1990). Clinical studies in ulcer caused by Helicobacter pylori infection: A. F. Carvalho et al., Aliment. Pharmacol. Ther. 12, 557 (1998); M. W. Whitehead et al., Helicobacter 5, 169 (2000); R. H. Phillips et al., ibid. 176.

Sinigrin CAS Registry Number: 3952-98-5 黑介子苷

CAS Name: 1-Thio-b-D-glucopyranose 1-[N-(sulfooxy)-3-butenimidate] monopotassium salt
Additional Names: sinigroside; myronate potassium; potassium myronate; allyl glucosinolate
Percent Compo...
Literature References: A b-glucopyranoside isolated from black mustard seeds and from the horseradish root Alliaria officinalis Andrz., Cruciferae: A. Bussy, J. Pharm. Chim. 26, 39 (1840); Gadamer, Arch. Pharm. 235, 44 (1897); Stoll, Seebeck, Helv. Chim. Acta 31, 1432 (1948). Structure: Ettlinger, Lundeen, J. Am. Chem. Soc. 78, 4173 (1956); 79, 1764 (1957). Hydrolysis: Ettlinger et al., Proc. Natl. Acad. Sci. USA 47, 1875 (1961). Crystal structure: Waser, Watson, Nature 198, 1297 (1963). Synthesis: Benn, Ettlinger, Chem. Commun. 1965, 445; A. Kjaer, Acta Chem. Scand. 22, 3324 (1968).