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

Tridemorph CAS Registry Number: 24602-86-6 异十三吗啉

CAS Name: 2,6-Dimethyl-4-tridecylmorpholine
Additional Names: N-tridecyl-2,6-dimethylmorpholine; 2,6-dimethyl-4-tridecyltetrahydro-1,4-oxazine
Percent Composition: C 76.70%, H 13.21%, N 4.71...
Literature References: Prepn: W. Sanne et al., BE 614214; eidem, US 3468885 (1962, 1969 both to BASF); K.-H. König et al., Angew. Chem. Int. Ed. 4, 336 (1965). Structure determn of two diastereomers: D. Kost, E. Gurfinkel, J. Chromatogr. 108, 207 (1975). Fungicidal activity: J. Kradel et al., Proc. 5th Brit. Insectic. Fungic. Conf., 16 (1969); in vitro activity comparison of tridemorph and commercial formulation Calixin: A. Kerkenaar, A. A. Sijpesteijn, Pestic. Biochem. Physiol. 12, 124 (1979). Uptake and distribution in barley: E.-H. Pommer et al., Proc. 5th Brit. Insectic. Fungic. Conf., 347 (1969); R. H. Waring, M. S. Wolfe, Pestic. Sci. 6, 169 (1975). Behavior in soil: S. Otto, N. Drescher, Proc. 7th Brit. Insectic. Fungic. Conf., 57 (1973). Metabolic fate in rats: D. R. Hawkins et al., Pestic. Sci. 5, 535 (1974); of Calixin: R. H. Waring, Xenobiotica 4, 717 (1974). Mode of action: A. Kerkenaar et al., Pestic. Biochem. Physiol. 12, 195 (1979). Comparison of toxicity of tridemorph and Calixin: J. Merkle et al., Teratology 29, 259 (1984). Field trials: P. Lakshmanan, S. Mohan, Pesticides 22, 27 (1988).

Carbamazepine CAS Registry Number: 298-46-4 卡马西平

CAS Name: 5H-Dibenz[b,f]azepine-5-carboxamide
Additional Names: 5-carbamoyl-5H-dibenz[b,f]azepineTrademarks: Biston (Slovakofarma); Calepsin (Orion); Carbatrol (Shire); Epitol (Teva); Finlepsin...
Literature References: Prepn: W. Schindler, US 2948718 (1960 to Geigy). Toxicity: E. G. Stenger, F. C. Roulet, Med. Exp. 11, 191 (1964). Review of GLC methods, pharmacokinetics and metabolism: S. Pynnönen, Ther. Drug Monit. 1, 409-431 (1979). Comprehensive description: H. Y. Aboul-Enein, A. A. Al-Badr, Anal. Profiles Drug Subs. 9, 87-106 (1980). Review of clinical use in pediatric seizures: J. T. Gilman, DICP Ann. Pharmacother. 25, 1109-1112 (1991); in trigeminal neuralgia: A. Sidebottom, S. Maxwell, J. Clin. Pharm. Ther. 20, 31-35 (1995).

Diflunisal CAS Registry Number: 22494-42-4 二氟尼柳

CAS Name: 2',4'-Difluoro-4-hydroxy-[1,1'-biphenyl]-3-carboxylic acid
Additional Names: 2',4'-difluoro-4-hydroxy-3-biphenylcarboxylic acid; 2',4'-difluoro-4-hydroxy-[1',1-diphenyl]-3-carboxylic ...
Literature References: Prepn: W. V. Ruyle et al., ZA 6701021; eidem, FR 1522570; eidem, US 3714226 (1968, 1968, 1973, all to Merck Co.); J. Hannah et al., J. Med. Chem. 21, 1093 (1978). Metabolism: P. J. DeSchepper et al., Br. J. Clin. Pharmacol. 4, 645P (1977). Clinical studies: J. A. Wojtulewski et al., Curr. Med. Res. Opin. 5, 562 (1978); J. A. Hicklin, ibid. 572; in sickle cell anemia: E. A. Oyewo, Clin. Trials J. 24, 249 (1987). Review of chemistry, pharmacology, clinical pharmacology: S. L. Steelman et al., ibid. 506-514. Comprehensive description: M. Cotton, R. A. Hux, Anal. Profiles Drug Subs. 14, 491-526 (1985). Review: Br. J. Clin. Pharmacol. 4, Suppl. 1, 1S-52S (1977); C. A. Winter et al., in Pharmacological and Biochemical Properties of Drug Substances vol. 3, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1981) pp 291-323. Comprehensive review of pharmacological properties and therapeutic use in pain: R. N. Brogden et al., Drugs 19, 84-106 (1980); Pharmacotherapy 3, no. 2, pt. 2, 1S-82S (1983).

Citiolone CAS Registry Number: 1195-16-0 3-乙酰氨基四氢-2-噻吩

CAS Name: 2-Acetamido-4-mercaptobutyric acid g-thiolactone
Additional Names: N-(tetrahydro-2-oxo-3-thienyl)acetamide; N-acetylhomocysteinethiolactone; a-acetamido-g-thiobutyrolactone; AHCTLTrad...
Literature References: Prepn: Wagner et al., DE 1134683 (1962 to Degussa, vorm Roessler), C.A. 58, 4648c (1963); Nakanishi et al., JP 62 16712 (1962 to Yoshitomi), C.A. 59, 11660h (1963); Takayananagi et al., JP 64 3420, C.A. 61, 3193h (1964); Ogino, Yasui, JP 65 1376, C.A. 62, 14822c (1965) (1964, 1965 both to Sumitomo). Chemistry: Benesch, Benesch, J. Am. Chem. Soc. 78, 1597 (1956); Laliberté et al., J. Chem. Soc. 1963, 2756. Pharmacology: E. -J. Kirnberger et al., Arzneim.-Forsch. 8, 72 (1958); Varga et al., ibid. 13, 1867 (1963).

Caprolactam CAS Registry Number: 105-60-2 己内酰胺

CAS Name: Hexahydro-2H-azepin-2-one
Additional Names: e-caprolactam; 2-oxohexamethylenimine; 2-ketohexamethylenimine; aminocaproic lactam
Percent Composition: C 63.68%, H 9.80%, N 12.38%, O ...
Literature References: Prepn: Wallach, Ann. 312, 187 (1900); 343, 43 (1905); Ruzicka et al., Helv. Chim. Acta 4, 477 (1921); Eck, Marvel, J. Biol. Chem. 106, 387 (1934); Marvel, Eck, Org. Synth. coll. vol. II, 371 (1943); Lazier, Rigby, US 2234566 (1941 to du Pont); Schlack, US 2249177 (1941 to I. G. Farben); DE 739953 (1943); DE 745224 (1943); P. Smith, J. Am. Chem. Soc. 70, 320 (1948); E. Schmitz et al., J. Prakt. Chem. 319, 274 (1977). Environmentally benign synthesis from cyclohexanone: J. M. Thomas, R. Raja, Proc. Natl. Acad. Sci. USA 102, 13732 (2005). Purification: Kampschmidt, US 2786052 (1957 to Stamicarbon N. V.). Stabilization with alkalies: Indest et al., US 2884414 (1959 to Vereinigte Glanzstoff-Fabriken). Toxicity study: H. F. Smyth et al., Am. Ind. Hyg. Assoc. J. 30, 470 (1969). Reviews: CIOS Repts. no. 22 and 31, File XXXIII/Synthetic Fiber Developments in Germany, parts I II; K. Kahr et al. in Ullmanns Encyklopädie der technischen Chemie vol. 9, E. Bartholome et al., Eds. (Verlag Chemie, Weinheim, 4th ed., 1975) pp 96-114.

Acetrizoate Sodium CAS Registry Number: 129-63-5 乙酰碘佐酸钠

CAS Name: 3-(Acetylamino)-2,4,6-triiodobenzoic acid sodium salt
Additional Names: 3-acetamido-2,4,6-triiodobenzoic acid sodium salt; acetrizoic acid sodium salt
Trademarks: Cystokon (Mallinc...
Literature References: Prepn: Wallingford et al., J. Am. Chem. Soc. 74, 4365 (1952); Wallingford, J. Am. Pharm. Assoc. Sci. Ed. 42, 721 (1953). Toxicity data: J. O. Hoppe et al., J. Pharmacol. Exp. Ther. 116, 394 (1956).

Piridocaine CAS Registry Number: 87-21-8 匹多卡因

CAS Name: 2-Piperidineethanol 2-aminobenzoate (ester)
Additional Names: anthranilic acid 2-(2-piperidyl)ethyl ester; 2-piperidineethanol anthranilate; b-(2-piperidyl)ethyl o-aminobenzoateTradem...
Literature References: Prepn: Walter, Fosbinder, J. Am. Chem. Soc. 61, 1713 (1939); US 2229533 (1941 to Maltbie Chem.).

Crufomate CAS Registry Number: 299-86-5 克芦磷酯

CAS Name: Methylphosphoramidic acid 2-chloro-4-(1,1-dimethylethyl)phenyl methyl ester
Additional Names: methylphosphoramidic acid 4-tert-butyl-2-chlorophenyl methyl ester; 4-tert-butyl-2-chloro...
Literature References: Prepn: Wasco et al., US 2929762 (1960 to Dow). Toxicity study: T. B. Gaines, Toxicol. Appl. Pharmacol. 14, 515 (1969). Anthelmintic activity in dairy cattle: E. T. Lyons et al., Am. J. Vet. Res. 43, 1072 (1982).

Ampyrone CAS Registry Number: 83-07-8 4-氨基安替比林

CAS Name: 4-Amino-1,2-dihydro-1,5-dimethyl-2-phenyl-3H-pyrazol-3-one
Additional Names: 4-aminoantipyrine; 4-amino-2,3-dimethyl-1-phenyl-3-pyrazolin-5-one; 1,5-dimethyl-2-phenyl-4-aminopyrazolon...
Literature References: Prepn: Waser, Helv. Chim. Acta 8, 117 (1925); Freedman, Sherndal, US 1877166 (1933 to H. A. Metz Labs.); Turpechen, Kallro, C.A. 36, 426 (1942); Takahashi, Ogyu, JP 54 3663 (1954 to Nippon New Drug), C.A. 50, 2687c (1956). Metabolite of aminopyrine, q.v.: E. S. Vesell et al., Clin. Pharmacol. Ther. 20, 661 (1976); G. F. Lockwood, J. B. Houston, J. Pharm. Pharmacol. 31, 787 (1979).

Sulfanitran CAS Registry Number: 122-16-7 磺胺硝苯

CAS Name: N-[4-[[(4-Nitrophenyl)amino]sulfonyl]phenyl]acetamide
Additional Names: 4'-[(p-nitrophenyl)sulfamoyl]acetanilide; N4-acetyl-N1-(p-nitrophenyl)sulfanilamide; 4-acetaminobenzenesulfon-4...
Literature References: Prepn: Webster, Powers, J. Am. Chem. Soc. 60, 1553 (1938); Kaufmann, Bückmann, Arch. Pharm. 279, 194 (1941); Shepherd, J. Org. Chem. 12, 275 (1947).