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

Chondrofoline CAS Registry Number: 31944-97-5

CAS Name: (1b)-6,6',7'-Trimethoxy-2,2'-dimethyltubocuraran-12'-ol
Additional Names: (R,R)-7-O-methylbebeerine; 7-O-methylcurine
Percent Composition: C 73.00%, H 6.62%, N 4.60%, O 15.77%
Literature References: Alkaloid isolated from the leaves of Chondrodendron platyphyllum (A. St. Hil.) Miers, Menispermaceae: King, J. Chem. Soc. 1940, 737. Structure, stereochemistry, NMR and mass spectrum: Baldas et al., Chem. Commun. 1971, 132. 13C-NMR: L. Koike et al., J. Org. Chem. 46, 2385 (1981).

Bicuculline CAS Registry Number: 485-49-4 (+)-荷包牡丹碱; 右旋荷包牡丹碱; 毕枯枯林; 山乌龟碱

CAS Name: (6R)-6-[(5S)-5,6,7,8-Tetrahydro-6-methyl-1,3-dioxolo[4,5-g]isoquinolin-5-yl]furo[3,4-e]-1,3-benzodioxol-8(6H)-one
Percent Composition: C 65.39%, H 4.66%, N 3.81%, O 26.13%
Literature References: Alkaloid naturally occurring in the d-form; found in Dicentra cucullaria (L.) Bernh., Adlumia fungosa (Ait.) Greene, Fumariaceae, and several Corydalis species: Manske, Can. J. Res. 7, 265 (1932); 8, 210, 407 (1933); 9, 436 (1933); Edwards, Handa, Can. J. Chem. 39, 1801 (1961). Synthesis of dl-form: Groenewoud, Robinson, J. Chem. Soc. 1936, 199. Resolution of isomers: Haworth et al., Nature 165, 529 (1950). Stereoisomer of adlumidine, q.v., and of capnoidine: Manske, J. Am. Chem. Soc. 72, 3207 (1950). Preliminary stereochemical studies: Safe, Moir, Can. J. Chem. 42, 160 (1964). Revised stereochemistry: Blaha et al., Collect. Czech. Chem. Commun. 29, 2328 (1964); Snatzke et al., Tetrahedron 25, 5059 (1969). Crystal and molecular structure: Gorinsky, Moss, J. Cryst. Mol. Struct. 3, 299 (1973). Shows GABA (q.v.) antagonist activity: Curtis et al., Nature 226, 1222 (1970).

Ergocryptinine CAS Registry Number: 511-10-4 (8alpha)-12'-羟基-5'alpha-异丁基-2'-异丙基麦角它曼-3',6',18-三酮

Additional Names: Ergokryptinine
Percent Composition: C 66.76%, H 7.18%, N 12.16%, O 13.90%
Literature References: Alkaloid pair isomeric with a- and b-ergocryptine, resp., but differing by an a-configuration at C-8. The literature prior to 1967 refers to a-ergocryptinine as ergocryptinine. Isolation, structure, separation and purification see ergocryptine. Production: Abe et al., US 2835675 (1958). Prepn of b-ergocryptinine from b-ergocryptine: Schlientz et al., Experientia 23, 991 (1967). Synthesis of a- and b-ergocryptinin: Stadler et al., Helv. Chim. Acta 52, 1549 (1969).

Mesembrine CAS Registry Number: 24880-43-1 松叶菊碱

CAS Name: (3aS-cis)-3a-(3,4-Dimethoxyphenyl)octahydro-1-methyl-6H-indol-6-one
Additional Names: 3a-(3,4-dimethoxyphenyl)tetrahydro-1-methyl-6(3aH)-indolinone
Percent Composition: C 70.56%, H...
Literature References: Alkaloid used in preparing Channa, a drug of Southwest Africa. Occurs naturally as the (-)-form. From Sceletium expansum L., S. tortuosum L., Aizoaceae: Hartwick, Zwicky, Apoth. Ztg. 29, 925 (1914); Rimington et al., J. Vet. Sci. Animal Ind. 9, 187 (1938), C.A. 32, 42799 (1938). Structure: Popelak et al., Naturwissenschaften 47, 156 (1960). Configuration: P. W. Jeffs et al., J. Am. Chem. Soc. 91, 3831 (1969). Synthesis of (±) form: Shamma, Rodriguez, Tetrahedron Lett. 1965, 4847; O. Hoshino et al., Heterocycles 10, 61 (1978); of (±)-form and trans isomer: Oh-Ishi, Kugita, Chem. Pharm. Bull. 18, 299 (1970). Synthesis of (+)-form: Yamada, Otani, Tetrahedron Lett. 1971, 1133; eidem, Chem. Pharm. Bull. 21, 2130 (1973). Stereoselective synthesis of (±)-form: Wijnberg, Speckamp, Tetrahedron Lett. 1975, 3963; eidem, Tetrahedron 34, 2579 (1978); S. F. Martin et al., J. Org. Chem. 44, 3391 (1979); S. Takano et al., Chem. Lett. 1981, 1385. Enantioselective synthesis of natural mesembrine: eidem, Tetrahedron Lett. 22, 4479 (1981). Biosynthesis: Jeffs et al., J. Am. Chem. Soc. 93, 3752 (1971); eidem, Chem. Commun. 1977, 60. Review of mesembrine alkaloids: A. Popelak, G. Lettenbauer in The Alkaloids vol. IX, R. H. F. Manske, Ed. (Academic Press, New York, 1967) pp 467-481; R. V. Stevens in The Total Synthesis of Natural Products vol. 3, J. ApSimon, Ed. (Wiley, New York, 1977) pp 443-453.

Germine CAS Registry Number: 508-65-6 4a,9-环氧瑟烷-3b,4,7a,14,15a,16b,20-七醇

CAS Name: (3b,4a,7a,15a,16b)-4,9-Epoxycevane-3,4,7,14,15,16,20-heptol
Percent Composition: C 63.63%, H 8.50%, N 2.75%, O 25.12%
Literature References: Alkamine present in many polyester alkaloids which occur in Veratrum and Zygadenus species. Isoln: Poethke, Pharm. Monatsh. 18, 77 (1937); idem, Arch. Pharm. 275, 571 (1937); Seiferle et al., J. Econ. Entomol. 35, 35 (1942); Klohs et al., J. Am. Chem. Soc. 75, 4925 (1953); Kupchan, Deliwala, ibid. 76, 5545 (1954); Myers et al., ibid. 77, 3348 (1955); 78, 1621 (1956). Structure and configuration: Kupchan, Narayanan, ibid. 81, 1913 (1959). Comparative toxicity: O. Krayer et al., J. Pharmacol. Exp. Ther. 82, 167 (1944).

Cafaminol CAS Registry Number: 30924-31-3 卡法醇胺

CAS Name: 3,7-Dihydro-8-[(2-hydroxyethyl)methylamino]-1,3,7-trimethyl-1H-purine-2,6-dione
Additional Names: 8-[(2-hydroxyethyl)methylamino]caffeine; 8-(b-oxyethyl)methylaminocaffeine; methylcof...
Literature References: Alkanolamine deriv of caffeine, q.v. Prepn: J. Klosa, DE 1085530; eidem, US 3094531 (1958, 1963 both to Delmar Chemicals Ltd.). Efficacy studies: E. Szirmai, Praxis 13, 412 (1969); R. Leypoldt, Therapiewoche 26, 3381 (1976). Bioavailability and absorption kinetics in humans: H. Walther, K. Kochler, Pharmazie 34, 375 (1979).

Eterobarb CAS Registry Number: 27511-99-5 依特比妥

CAS Name: 5-Ethyl-1,3-bis(methoxymethyl)-5-phenyl-2,4,6(1H,3H,5H)-pyrimidinetrione
Additional Names: 5-ethyl-1,3-bis(methoxymethyl)-5-phenylbarbituric acid; N,N'-dimethoxymethylphenobarbital; e...
Literature References: Alkoxymethyl deriv of phenobarbital, q.v., reported to have little or no hypnotic activity. Prepn: C. M. Samour, J. A. Vita, DE 1939987; J. A. Vita, US 3595862 (1970, 1971 both to Kendall); C. M. Samour et al., J. Med. Chem. 14, 187 (1971); J. Gal, J. Pharm. Sci. 68, 1562 (1979). Spectrophotographic and polarographic analysis: M. Romer et al., Anal. Chim. Acta 88, 261 (1977). Pharmacologic study: J. A. Vida, M. L. Hasker, J. Med. Chem. 16, 602 (1973). Metabolism: M. A. Goldberg et al., Ann. Neurol. 5, 121 (1979). Efficacy in febrile convulsions: R. M. Julien, G. G. Fowler, Neuropharmacology 16, 719 (1977).

Improsulfan CAS Registry Number: 13425-98-4 英丙舒凡

CAS Name: 3,3'-Iminobis-1-propanol dimethanesulfonate (ester)
Additional Names: N,N-bis(3-methylsulfonyloxypropyl)amine; bis(3-mesyloxypropyl)amine
Percent Composition: C 33.21%, H 6.62%, N ...
Literature References: Alkylating agent related to busulfan, q.v. Prepn and antitumor activity of the hydrochloride: M. M. El-Merzabani, Y. Sakurai, Gann 56, 589 (1965), C.A. 64, 8793b (1965); Y. Sakurai, JP 67 26616 (1967), C.A. 69, 51596f (1968). Prepn of the tosylate: M. Nakanishi et al., DE 2059377 (1971 to Yoshitomi), C.A. 75, 63127r (1972). Absorption, distribution, excretion, metabolism: Y. Kato et al., Yakugaku Zasshi 94, 1107 (1974), C.A. 82, 38441a (1975). Pharmacology: N. Brock, J. Kuhlmann, Arzneim.-Forsch. 24, 1139 (1974); H. Imamura et al., Oyo Yakuri 9, 861 (1975), C.A. 84, 12492j (1976). Antitumor effect: T. Okumoto et al., Chem. Pharm. Bull. 25, 3003 (1977); T. Iwaguchi, H. Kitagawa, Gann 69, 123 (1968), C.A. 89, 157282 (1978). Clinical study: S. J. Altman et al., Cancer 35, 1145 (1975). Toxicity study: N. Rakieten et al., U.S. NTIS Report PB-196468 (1970) 17 pp, C.A. 75, 47359n (1971). Mutagenicity study: W. F. Benedict et al., Cancer Res. 37, 2209 (1977).

Procarbazine CAS Registry Number: 671-16-9 甲基苄肼

CAS Name: N-(1-Methylethyl)-4-[(2-methylhydrazino)methyl]benzamide
Additional Names: N-isopropyl-a-(2-methylhydrazino)-p-toluamide; N-4-isopropylcarbamoylbenzyl-N'-methylhydrazine; p-(N1-methyl...
Literature References: Alkylating agent. Prepn: BE 618638; W. Bollag et al., US 3520926 (1962, 1970 to Hoffmann-La Roche). Toxicity data: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Comprehensive description: R. J. Rucki, Anal. Profiles Drug Subs. 5, 403-427 (1976). HPLC determn in plasma: X. He et al., J. Chromatogr. B 799, 281 (2004). Review of clinical experience in hematological malignancies: M. Massoud et al., Eur. J. Cancer 40, 1924-1927 (2004).

Dipin CAS Registry Number: 738-99-8 1,4-二(N,N'-二亚乙基磷酰胺)哌嗪

CAS Name: 1,4-Bis[bis(1-aziridinyl)phosphinyl]piperazine
Additional Names: 1,4-piperazinediylbis[bis(1-aziridinyl)phosphine oxide]; piperazine-1,4-bis(N,N'-diethylenephosphonediamide); tetraeth...
Literature References: Alkylating agent; exptl antineoplastic. Prepn: Kropacheva et al., Zh. Obshch. Khim. 30, 3584 (1960), C.A. 55, 18695c (1961). Spectrophotometric determn: L. Kh. Kartashova, E. M. Salomatin, Farmatsiya (Moscow) 33, 72 (1983), C.A. 102, 119736j (1985). Metabolism in rats: V. V. Chistyakov et al., Khim. Farm. Zh. 21, 398 (1987), C.A. 107, 146734s (1987).