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

Cloricromen CAS Registry Number: 68206-94-0 氯克罗孟

CAS Name: [[8-Chloro-3-[2-(diethylamino)ethyl]-4-methyl-2-oxo-2H-1-benzopyran-7-yl]oxy]acetic acid ethyl ester
Additional Names: ethyl [[8-chloro-3-[2-(diethylamino)ethyl]-4-methyl-2-oxo-2H-1-b...
Literature References: Derivative of coumarin, q.v. Prepn: F. della Valle, BE 871315; idem, US 4452811 (1979, 1984 both to Fidia). In vivo studies of activity as coronary vasodilator: F. Aporti et al., Pharmacol. Res. Commun. 10, 469 (1978); as inhibitor of platelet aggregation: M. Prosdocimi et al., Thromb. Res. 39, 399 (1985). Pharmacology in human platelets: R. A. Travagli et al., ibid. 54, 327 (1989). Mechanism of action: S. Porcellati et al., Agents Actions 29, 364 (1990).

Fluticasone Propionate CAS Registry Number: 80474-14-2 氟替卡松丙酸酯

CAS Name: (6a,11b,16a,17a)-6,9-Difluoro-11-hydroxy-16-methyl-3-oxo-17-(1-oxopropoxy)androsta-1,4-diene-17-carbothioic acid S-(fluoromethyl) ester
Additional Names: S-fluoromethyl 6a,9a-difluoro...
Literature References: Derivative of flumethasone, q.v. Prepn: NL 81 00707; G. H. Phillipps et al., US 4335121 (1981, 1982 both to Glaxo). Series of articles on structure-activity, pharmacology and clinical studies: Respir. Med. 84, Suppl. A, 19-35 (1990). Clinical trials in allergic rhinitis: E. O. Meltzer et al., J. Allergy Clin. Immunol. 86, 221 (1990). Evaluation in untreated celiac disease: H. C. Mitchison et al., Gut 32, 260 (1991). Clinical trials in COPD: P. L. Paggiaro et al., Lancet 351, 773 (1998); P. S. Burge et al., Br. Med. J. 320, 1297 (2000). Clinical comparison with zafirlukast, q.v., in persistant asthma: J. H. Brabson et al., Am. J. Med. 113, 15 (2002).

Oxaceprol CAS Registry Number: 33996-33-7 N-乙酰基-L-羟脯氨酸

CAS Name: (4R)-1-Acetyl-4-hydroxy-L-proline
Additional Names: 4-hydroxy-N-acetylproline; 1-acetyl-4-hydroxy-2-pyrrolidinecarboxylic acidTrademarks: Jonctum (Hoechst)
Percent Composition: C 4...
Literature References: Derivative of hydroxyproline having anti-inflammatory activity. Prepn: R. L. M. Synge, Biochem. J. 33, 1924 (1939); J. J. Kolb, G. Toennies, J. Biol. Chem. 144, 193 (1942); O. Leonardo et al., DE 2301358 corresp to US 3860607 (1973, 1975 to Richardson-Merrell). Elucidation of cyclic conformation and cis/trans isomerism about the amide bond: T. Prange et al., Biochem. Biophys. Res. Commun. 61, 104 (1974). Crystal structure: M. Hospital et al., Biopolymers 18, 1141 (1979). In crystals, the acetyl group is in the trans conformation and the ring is puckered. The trans form is more stable than the cis form in solutions: W. A. Thomas, M. K. Williams, J. Chem. Soc. Chem. Commun. 1972, 994. Anti-inflammatory and wound-healing activity in animals: P. Coirre, B. Coirre, GB 1246141 (1971) related to P. Coirre et al., US 3891765 and US 3932638 (1975, 1976 both to Franco Chimie). Clinical studies of use in several rheumatic conditions: P. Grellat, Rhumatologie 27, 223 (1975); in degenerative joint disease, R. Schubotz, L. Hausmann, Therapiewoche 27, 4248 (1977); in treatment of burns, tumors and other wounds (applied locally): Y. Privat, Gaz. Med. Fr. 84, 618 (1977).

Piketoprofen CAS Registry Number: 60576-13-8 吡酮洛芬

CAS Name: 3-Benzoyl-a-methyl-N-(4-methyl-2-pyridinyl)benzeneacetamide
Additional Names: m-benzoyl-N-(4-methyl-2-pyridyl)hydratropamide; 2-(3-benzoylphenyl)-N-(4-methyl-2-pyridyl)propionamide Literature References: Derivative of ketoprofen, q.v. used topically as cream or aerosol. Prepn: R. G. W. Spickett et al., GB 1436502 (1976 to Antonio Gallardo, S.A.). Pharmacology and clinical efficacy: E. Tarrus et al., 2nd Eur. Congr. Biopharm. Pharmacokinet. 1, 483 (1984).

Hydroxypropyl Methylcellulose CAS Registry Number: 9004-65-3 羟丙基甲基纤维素

CAS Name: Cellulose 2-hydroxypropyl methyl ether
Additional Names: hypromellose; HPMC
Trademarks: Artelac (Mann); Benecel MP (Hercules); GenTeal (Novartis); Gonak (Akorn); Goniosol (Novartis...
Literature References: Derivative of methylcellulose, q.v., that also contains 3-12% hydroxypropyl substitution. Prepn: A. B. Savage, US 2949452 (1960 to Dow). Review of chemistry, physical properties and use: idem, Encyclopedia of Polymer Science and Technology vol. 3 (Interscience, New York, 1965); pp 496-511; G. K. Greminger, A. B. Savage, Industrial Gums, R. L. Whistler, Ed. (Academic Press, New York, 1973) pp 619-647. Clinical efficacy as ocular lubricant in Sjogren's syndrome: I. Toda et al., Cornea 15, 120 (1996); in contact lens solutions: P. A. Simmons et al., CLAO J. 27, 192 (2001). Review of production and uses in foods: P. de Mariscal, D. A. Bell in Handbook of Fat Replacers, S. Roller, S. A. Jones, Eds. (CRC Press, Boca Raton FL, 1996) pp 145-159. Review of drug release from HPMC-based pharmaceutical systems: J. Siepmann, N. A. Peppas, Adv. Drug Delivery Rev. 48, 139-157 (2001).

Tiamulin CAS Registry Number: 55297-95-5 泰妙菌素

CAS Name: (3aS,4R,5S,6S,8R,9R,9aR,10R)-[[2-(Diethylamino)ethyl]thio]acetic acid 6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3aH-cyclopentacycloocten-8-yl ester
Addition...
Literature References: Derivative of pleuromutilin, q.v. Prepn: H. Egger, DE 2248237 corresp to US 3919290 (1973, 1975 both to Sandoz); H. Egger, H. Reinshagen, J. Antibiot. 29, 915 (1976). Biosynthesis: F. Knauseder, E. Brandl, ibid. 125. In vitro activity: H. Werner et al., ibid. 31, 756 (1978). Metabolism: J. Dreyfuss et al., ibid. 32, 496 (1979). Effect vs Mycoplasma: C. O. Baughn et al., Avian Dis. 22, 620 (1978); R. F. Goodwin, Vet. Rec. 104, 194 (1979). Mechanism of action: G. Högenauer in Antibiotics vol. 5(pt. 1), F. E. Hahn, Ed. (Springer-Verlag, New York, 1979) pp 344-360. Treatment of swine dysentery: M. D. Anderson, Vet. Med. Small Anim. Clin. 78, 98 (1983).

Limaprost CAS Registry Number: 74397-12-9 利马前列素

CAS Name: (2E,11a,13E,15S,17S)-11,15-Dihydroxy-17,20-dimethyl-9-oxoprosta-2,13-dien-1-oic acid
Additional Names: 17S,20-dimethyl-trans-2,3-didehydro-PGE1; 9-oxo-11a,15a-dihydroxy-17S,20-dimethy...
Literature References: Derivative of prostaglandin E1, q.v. Prepn: M. Hayashi et al., DE 3002677 (1980 to Ono); eidem, US 4294849 (1981 to Warner-Lambert). Cardiovascular pharmacology in animals: T. Tsuboi et al., Arch. Int. Pharmacodyn. 247, 89 (1980). Effect on smooth muscle in vitro: P. G. Adaikan, S. M. M. Karim, Prostaglandins Med. 6, 449 (1981). Coronary vasodilating effects in primates: S. R. Kottegoda et al., Prostaglandins Leukotrienes Med. 8, 343 (1982). Clinical hemodynamics in chronic lung disease: T. Ishizaki et al., Chest 85, 382 (1984).

Methabenzthiazuron CAS Registry Number: 18691-97-9 甲基苯噻隆

CAS Name: N-2-Benzothiazolyl-N,N'-dimethylurea
Additional Names: 1-(2-benzothiazolyl)-1,3-dimethylurea; metabenzthiazuron; MBUTrademarks: Tribunil (Bayer)
Percent Composition: C 54.28%, H 5....
Literature References: Derivative of urea. Prepn and use as pre-emergence herbicide: N. E. Searle, US 2756135 (1956 to du Pont). Use as pre- and post-emergence herbicide in wheat and barley: H. Hack et al., GB 1085430 (1967 to Bayer). Herbicidal properties: H. Hack, Pflanzenschutz-Nachr. 22, 331 (1969). Toxicity studies: G. Kimmerle, E. Löser, ibid. 351. Use in winter cereals: D. C. Clark et al., Proc. 12th Brit. Weed Control Conf. 163 (1974). Mode of action: G. F. Collet, Weed Res. 9, 340 (1969). Long-term effect on soil: P. L. Huge, Pflanzenschutz-Nachr. 34, 97 (1981). Brief review: P. Lours, Def. Veg. 24, 91 (1970).

Sodium Diacetate CAS Registry Number: 126-96-5 双乙酸钠

Additional Names: Sodium acid acetate
Trademarks: Dykon
Percent Composition: C 33.81%, H 4.97%, Na 16.18%, O 45.04%
Literature References: Described as a "bound" compd of sodium acetate and acetic acid.

Oxychlorosene CAS Registry Number: 8031-14-9 奥昔氯生

Additional Names: Monoxychlorosene
Trademarks: Clorpactin (Guardian); Clorpactin XCB (Guardian)
Percent Composition: C 59.02%, H 8.67%, Cl 8.71%, O 15.72%, S 7.88%
Literature References: Described as a buffered organic hypochlorous acid derivative with slightly acid pH. Contains a long chain hydrocarbon (surface-active agent). The chain (14 carbons) may be branched or straight but actually consists of a constant mixture having predominantly the straight chain. The hydrocarbon chain also has a phenyl substituent which in turn holds a sulfonic acid group. The complex corresponds to a formula: HO3S-C6H4-(C14H29).HOCl.