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

Entecavir CAS Registry Number: 142217-69-4 恩替卡韦

CAS Name: 2-Amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one
Percent Composition: C 51.98%, H 5.45%, N 25.26%, O 17.31%
Literature References: Deoxyguanine nucleoside analog; inhibits hepatitis B virus (HBV) DNA polymerase. Prepn: R. Zahler, W. A. Slusarchyk, EP 481754; eidem, US 5206244 (1992, 1993 both to Squibb); G. S. Bisacchi et al., Bioorg. Med. Chem. Lett. 7, 127 (1997). In vitro antiviral activity: S. F. Innaimo et al, Antimicrob. Agents Chemother. 41, 1444 (1997). Review of pharmacology and clinical experience: P. Honkoop, R. A. de Man, Expert Opin. Invest. Drugs 12, 683-688 (2003); T. Shaw, S. Locarnini, Expert Rev. Anti Infect. Ther. 2, 853-871 (2004). Clinical comparisons with lamivudine in chronic hepatitis B: T.-T. Chang et al., N. Engl. J. Med. 354, 1001 (2006); C.-L. Lai et al., ibid. 1011.

Nitracrine CAS Registry Number: 4533-39-5 尼曲吖啶

CAS Name: N,N-Dimethyl-N'-(1-nitro-9-acridinyl)-1,3-propanediamine
Additional Names: 9-[[3-(dimethylamino)propyl]amino]-1-nitroacridine
Percent Composition: C 66.65%, H 6.21%, N 17.27%, O 9....
Literature References: Deriv of acridine, q.v., with cytostatic and cytotoxic properties. Prepn: FR 1458183 (1966 to Polfa), C.A. 68, 39493s (1968); A. Ledochowski, B. Stefanska, Rocz. Chem. 40, 301 (1966), C.A. 65, 2219b (1966). Pharmacological studies: J. Gieldanowski et al., Arch. Immunol. Ther. Exp. 20, 399 (1972); eidem, ibid. 419. Mechanism of action: J. Konopa et al., Mater. Med. Pol. 8, 258 (1976). Cytotoxicity study: I. Szumiel, M. Walicka, Neoplasma 27, 697 (1980). DNA binding activity: L. Szmigiero, M. Gniazdowski, Arzneim.-Forsch. 31, 1875 (1981). Comprehensive review: M. Gniazdowski et al. in Antibiotics Vol. V, part 2, F. E. Hahn, Ed. (Springer-Verlag, New York, 1979) pp 275-297.

Rimantadine CAS Registry Number: 13392-28-4 1-金刚烷乙胺

CAS Name: a-Methyltricyclo[3.3.1.13,7]decane-1-methanamine
Additional Names: a-methyl-1-adamantanemethylamine; remantadin(e)
Percent Composition: C 80.38%, H 11.81%, N 7.81%
Literature References: Deriv of adamantane, q.v. Prepn: NL 6408505; W. W. Prichard, US 3352912 (1965, 1967 both to du Pont). Antiviral activity: A. Tsunoda et al., Antimicrob. Agents Chemother. 1965, 553. Effects on influenza in mice: J. W. McGahen et al., Ann. N.Y. Acad. Sci. 173, 557 (1970). Mechanism of action study: A. Bukrinskaya et al., Arch. Virol. 66, 275 (1980); eidem, J. Gen. Virol. 60, 49 (1982). Pharmacokinetics in humans: R. J. Wills et al., Antimicrob. Agents Chemother. 31, 826 (1987). Clinical trial in prophylaxis of influenza A infection: R. Dolin et al., N. Engl. J. Med. 307, 580 (1982). Comparative toxicity of rimantadine and amantadine in healthy adults: F. G. Hayden et al., Antimicrob. Agents Chemother. 19, 226 (1981). Controlled study of CNS effects: V. M. Millet et al., ibid. 21, 1 (1982). Review of studies in the USSR on exptl and clinical pharmacology: D. M. Zlydnikov et al., Rev. Infect. Dis. 3, 408-421 (1981).

Fenproporex CAS Registry Number: 15686-61-0

CAS Name: 3-[(1-Methyl-2-phenylethyl)amino]propanenitrile
Additional Names: (±)-3-[(a-methylphenethyl)amino]propionitrile; (±)-N-2-cyanoethylamphetamine
Percent Composition: C 76.5...
Literature References: Deriv of amphetamine, q.v. Prepn: FR M4364; P. Pohrbach, J. Blum, US 3485924 (1966, 1969 both to Bottu). Pharmacological studies: B. M. Beecham et al., J. Pharm. Pharmacol. 23, 140 (1971); A. H. Beckett et al., ibid. 24, 194 (1972). Peripheral effects in human and rat adipose tissue: M. Dubost et al., Br. J. Pharmacol. 58, 436P (1976). Chromatographic identification of amphetamine in urine of patients treated with fenproporex: R. B. Sznelvar, Eur. J. Toxicol. Environ. Hyg. 8, 5 (1975). Clinical trial: G. Hertel, W. Fallot-Burghardt, Fortschr. Med. 96, 2380 (1978).

Tolfenamic Acid CAS Registry Number: 13710-19-5 托芬那酸

CAS Name: 2-[(3-Chloro-2-methylphenyl)amino]benzoic acid
Additional Names: N-(3-chloro-o-tolyl)anthranilic acid; N-(2-methyl-3-chlorophenyl)anthranilic acidTrademarks: Clotam (GEA); Tolfedine (...
Literature References: Deriv of anthranilic acid, related structurally to mefenamic and flufenamic acids, q.q.v. Prepn: NL 6600251 (1966 to Gea A/S), C.A. 66, 2377 (1967); R. A. Scherrer, F. W. Short, US 3313848 (1967 to Parke, Davis). Inhibition of prostaglandin biosynthesis: I. B. Linden et al., Scand. J. Rheumatol. 5, 129 (1976). HPLC determn: F. Nielsen-Kudsk, Acta Pharmacol. Toxicol. 47, 267 (1980). Metabolism: T. Kuninaka et al., Yakugaku Zasshi 101, 232 (1981), C.A. 95, 168 (1981). Human pharmacokinetics: P. Pentikaeinen et al., Eur. J. Clin. Pharmacol. 19, 359 (1981). Pharmacological studies: S. Yamashita et al., Toho Igakkai Zasshi 28, 76-105 (1981), C.A. 95, 16183, 180846 (1981). Clinical study: V. Rejholec et al., Scand. J. Rheumatol. Suppl. 33, 50 (1980); Suppl. 36, 1 (1980).

Oxamarin CAS Registry Number: 15301-80-1 奥沙香豆素

CAS Name: 6,7-Bis[2-(diethylamino)ethoxy]-4-methyl-2H-1-benzopyran-2-one
Additional Names: 6,7-bis[2-(diethylamino)ethoxy]-4-methylcoumarin
Percent Composition: C 67.66%, H 8.78%, N 7.17%, O...
Literature References: Deriv of a-pyrone, related structurally to sulmarin, q.v. Prepn: E. Massarani, Farmaco Ed. Sci. 12, 691 (1957); G. Cavallini, E. Massarani, US 2895963 (1959 to Maggioni); E. Massarani et al., J. Med. Pharm. Chem. 3, 231 (1961). Comparative study in treatment of varicose syndrome: G. Frantoli et al., Panminerva Med. 14, 290 (1972), C.A. 78, 92741 (1973). Transcutaneous absorption: G. Ciaceri, P. Marini, Boll. Chim. Farm. 111, 321 (1972). Cardiovascular, intestinal smooth muscle effects: eidem, G. Ital. Patol. Sci. Affini 19, 11 (1972), C.A. 81, 130823 (1974). Anti-inflammatory action: eidem, ibid. 1, C.A. 81, 130952 (1974).

Etersalate CAS Registry Number: 62992-61-4 依特柳酯

CAS Name: 2-(Acetyloxy)benzoic acid 2-[4-(acetylamino)phenoxy]ethyl ester
Additional Names: 2-(4-acetamidophenoxy)ethyl 2-acetoxybenzoate; eterilate; etherylate; eterylate
Trademarks: Daital...
Literature References: Deriv of aspirin. Prepn: C. S. Letelier, F. C. Grafulia, DE 2538206; eidem, US 4014921 (both 1977 to Alter); C. S. Letelier et al., Arch. Farmacol. Toxicol. 4, 153 (1978). Effect on in vitro platelet function in human plasma: M. P. Ortega et al., ibid. 6, 31 (1980). In vivo effects on primary immune response: I. Barasoain et al., Immunopharmacology 2, 293 (1980). Comparative toxicity study and gastric tolerance: S. Alonso et al., Arch. Farmacol. Toxicol. 4, 349 (1978).

Peplomycin CAS Registry Number: 68247-85-8 派来霉素

CAS Name: N1-[3-[[(1S)-1-Phenylethyl]amino]propyl]bleomycinamide
Additional Names: N1-[3-[[(S)-a-methylbenzyl]amino]propyl]bleomycinamide; pepleomycinPercent Composition: C 49.72%, H 6.02%, N 1...
Literature References: Deriv of bleomycin, q.v. with cytostatic activity and less pulmonary toxicity than the natural bleomycin mixture. Prepn of the (R,S)-form: H. Umezawa et al., US 3846400 (1974 to Microbiochem. Res. Found.); of the (S)-form: T. Takita et al., DE 2828933; eidem, US 4195018 (1979, 1980 both to Nippon Kayaku); W. Tanaka et al., Heterocycles 13, 469 (1979). Biological study of degradation products: K. Takahashi et al., J. Antibiot. 32, 36 (1979). General pharmacology: Y. Ishii et al., Jpn. J. Antibiot. 31, 886 (1978), C.A. 91, 215c (1979). Absorption, distribution, excretion, metabolism: H. Takayama et al., ibid. 895, C.A. 91, 32580j (1979). Properties and stability: A. Fuji et al., Iyakuhin Kenkyu 10, 197 (1979), C.A. 91, 9408a (1979). Effect in prostatic cancer: T. Niijima, K. Koiso, Scand. J. Respir. Dis. Suppl. 55, 177 (1980). Relative pulmonary toxicity: B. I. Sikic et al., Cancer Treat. Rep. 64, 659 (1980). Acute toxicity study: K. Ito et al., Jpn. J. Antibiot. 31, 719 (1978), C.A. 91, 68461k (1979). Review of clinical studies: S. Oko, Recent Results Cancer Res. 74, 163 (1980).

Colchiceine CAS Registry Number: 477-27-0 原水仙碱

CAS Name: N-[(7S)-5,6,7,9-Tetrahydro-10-hydroxy-1,2,3-trimethoxy-9-oxobenzo[a]heptalen-7-yl]acetamide
Additional Names: 7-acetamido-10-hydroxy-1,2,3-trimethoxy-6,7-dihydrobenzo[a]heptalen-9(5H)...
Literature References: Deriv of colchicine, q.v., isolated from Colchicum autumnale L., Liliaceae: Santavy, Macák, Collect. Czech. Chem. Commun. 19, 805 (1954). Toxicity data: B. Goldberg et al., Cancer 3, 124 (1950). Structure and synthesis: Nakamura, Chem. Pharm. Bull. 10, 299 (1962). Circular dichroism: J. Hrbek et al., Collect. Czech. Chem. Commun. 47, 2258 (1982). Effect on antibody response induced in vitro: J. Sterzl et al., Folia Microbiol. 27, 256 (1982).

Enocitabine CAS Registry Number: 55726-47-1 依诺他滨

CAS Name: N-(1-b-D-Arabinofuranosyl-1,2-dihydro-2-oxo-4-pyrimidinyl)docosanamide
Additional Names: N(4)-behenoyl-1-b-D-arabinofuranosylcytosine; behenoylcytosine arabinoside; BH-ACTrademarks: S...
Literature References: Deriv of cytarabine, q.v. Prepn: T. Ishida et al., DE 2426304; eidem, US 3991045 (1975, 1976 both to Asahi); M. Akiyama et al., Chem. Pharm. Bull. 26, 981 (1978). Antitumor activity: M. Aoshima et al., Cancer Res. 36, 2726 (1976); eidem, ibid. 37, 2481 (1977). Distribution, excretion: M. Fukama et al., Gan to Kagaku Ryoho 7, 2109 (1980), C.A. 95, 35186 (1981). Effect and mode of action: T. Kataoka, Y. Sakurai, Recent Results Cancer Res. 70, 147 (1980). Pharmacological and clinical studies: K. Yamada et al., ibid. 219.