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

Polyestradiol Phosphate CAS Registry Number: 28014-46-2

CAS Name: Estradiol phosphate polymer
Additional Names: PEP
Trademarks: Estradurin (Kabi)
Literature References: Polymeric ester of phosphoric acid and estradiol. Mol wt ~26,000. Prepn: Diczfalusy, Endocrinology 54, 471 (1954); Fernö et al., Acta Chem. Scand. 12, 1675 (1958); Diczfalusy et al., US 2928849 (1960 to AB Leo). Clinical pharmacology: P. O. Gunnarsson, B. J. Norlén, Prostate 13, 299 (1988). Clinical trial in prostatic carcinoma: J. Aro, ibid. 18, 131 (1991).

Sevelamer CAS Registry Number: 52757-95-6 司维拉姆

CAS Name: 2-Propen-1-amine polymer with (chloromethyl)oxirane
Additional Names: allylamine polymer with 1-chloro-2,3-epoxypropane; allylamine-epichlorohydrin copolymer; poly(allylamin-co-N,N'-d...
Literature References: Polymeric non-absorbed phosphate binder consisting of polyallylamine crosslinked with epichlorohydrin to form a hydrogel where 40% of the amines are protonated. Follows the general formula of (C3H7N.C3H5ClO)n. Binds dietary phosphate leading to increased fecal excretion, decreased absorption and decreased serum phosphorous levels. Prepd not claimed: S. R. Holmes-Farley et al., WO 9505184; eidem, US 5496545 (1995, 1996 both to GelTex). Mechanism of action: S. R. Holmes-Farley et al., J. Macromol. Sci. Pure Appl. Chem. A36, 1085 (1999). Determn of phosphate binding capacity: J. R. Mazzeo et al., J. Pharm. Biomed. Anal. 19, 911 (1999). Clinical studies in end stage renal disease: E. A. Slatopolsky et al., Kidney Int. 55, 299 (1999).

Dehydroacetic Acid CAS Registry Number: 520-45-6 脱氢乙酸

CAS Name: 3-Acetyl-6-methyl-2H-pyran-2,4(3H)-dione
Additional Names: 2-acetyl-5-hydroxy-3-oxo-4-hexenoic acid d-lactone; methylacetopyronone; DHA
Percent Composition: C 57.14%, H 4.80%, O 38...
Literature References: Polymerization product of ketene: Steele et al., J. Org. Chem. 14, 460 (1949). From ethyl acetoacetate: Arndt, Org. Synth. coll. vol. III, 231 (1955). Toxicity study: H. C. Spencer et al., J. Pharmacol. Exp. Ther. 99, 57 (1950). Series of articles on toxicity studies, pharmacology, mechanism of action, absorption, distribution, renal action: ibid. 57-111.

Hemozoin CAS Registry Number: 39404-00-7

Additional Names: b-Hematin; malaria pigment; haemozoin; HZ
Literature References: Polymerized heme produced as a detoxification response by malaria parasites and by blood-sucking insects. It is the end product of hemoglobin digestion in intraerythrocytic malaria parasites. Constituents include hematin and protein but the exact composition remains unclear. Identification: T. Carbone, Giorn. Regia. Acad. Med. Torino 39, 901 (1891). Biochemical characterization: P. Goldie et al., Am. J. Trop. Med. Hyg. 43, 584 (1990). Identification in tissue: A D. Sullivan, S. R. Meshnick, Parasitol. Today 12, 161 (1996); of formation in insects: M. F. Oliveira et al., Nature 400, 517 (1999). Depression of cellular immunity: F. Turrini et al., ibid. 9, 297 (1993). Effect of antimalarials on depolymerization: A. V. Pandey, B. L. Tekwani, FEBS Lett. 402, 236 (1997). Review: P. Arese, E. Schwarzer, Ann. Trop. Med. Parasitol. 91, 501 (1997).

Thiostrepton CAS Registry Number: 1393-48-2 硫链丝菌素

Trademarks: Bryamycin (BMS); Thiactin
Percent Composition: C 51.94%, H 5.15%, N 15.98%, O 17.30%, S 9.63%
Literature References: Polypeptide antibiotic contg sulfur. Produced by Streptomyces azureus isolated from New Mexican soil: Pagano et al., Antibiot. Annu. 1955-56, 554; Vandeputte, Dutcher, ibid. 560; GB 795570 (1958); Donovick et al.; Platt, US 2982689; US 2982698 (1961 all to Olin Mathieson). Structure studies: Bodanszky et al., J. Am. Chem. Soc. 84, 2003 (1962); 86, 2478 (1964); Anderson et al., Nature 225, 233 (1970). Total structure determn: K. Tori et al., Tetrahedron Lett. 1976, 185; eidem, J. Antibiot. 32, 1072 (1979). 13C-NMR study: eidem, ibid. 34, 124 (1981). Total synthesis: K. C. Nicolaou et al., Angew. Chem. Int. Ed. 43, 5087, 5092 (2004). Mode of action as an inhibitor of protein synthesis: Cannon, Burns, FEBS Lett. 18, 1 (1971); Cundliffe, Biochem. Biophys. Res. Commun. 44, 912 (1971). Identity with thiactin: Bodanszky et al., J. Antibiot. 16A, 76 (1963). Comprehensive description: K. Florey, Anal. Profiles Drug Subs. 7, 423-444 (1978). Review: Pestka, Bodley, in Antibiotics vol. 3, J. W. Corcoran, F. E. Hahn, Eds. (Springer-Verlag, New York, 1975) pp 551-573; E. Cundliffe, ibid. vol. 5 (pt. 1), F. E. Hahn, Ed. (1979) pp 329-343.

Tyrothricin CAS Registry Number: 1404-88-2 短杆菌素

Additional Names: Dubos crude crystals
Trademarks: Hydrotricine (RPR); Dermotricine (Bellon); Tyri 10 (Lindopharm); Tyrosur (Engelhard KG)
Literature References: Polypeptide antibiotic mixture extracted from cultures of soil bacilli belonging to the Tyrothrix group of bacteria. Usually obtained by extracting acidified cultures of Bacillus brevis with alc and precipitating with NaCl soln. Surface, submerged, and aerated cultures are used. Tyrothricin contains from 10 to 20% gramicidin and from 40 to 60% tyrocidine. Solubility data: Weiss et al., Antibiot. Chemother. 7, 374 (1957). Function in the sporulation process: Sarkar, Paulus, Nature New Biol. 239, 228 (1972). Toxicity data: H. Sous et al., Arzneim.-Forsch. 7, 98 (1957).

Amphomycin CAS Registry Number: 1402-82-0 安福霉素

Additional Names: Amfomycin; glumamycin
Percent Composition: C 53.98%, H 7.11%, N 14.11%, O 24.80%
Literature References: Polypeptide antibiotic modified at the amino terminus with a fatty acid moiety; active against gram positive bacteria. Produced by Streptomyces canus from soil collected near Syracuse, N.Y.: B. Heinemann et al., Antibiot. Chemother. 3, 1239 (1953). Production: eidem, US 3126317 (1964 to Bristol-Myers). Structure and identity with glumamycin: M. Bodanszky et al., J. Am. Chem. Soc. 95, 2352 (1973). Pharmacology and toxicity: D. E. Tisch et al., Antibiot. Annu. 1954-1955, 1011. Mechanism of action: H. Tanaka et al., Biochem. Biophys. Res. Commun. 86, 902 (1979). Use to improve feed efficiency in ruminant animals: M. Gordon, G. J. Christie, DE 3027370; eidem, US 4414206 (1981, 1983 both to Bristol-Myers).

Enviomycin CAS Registry Number: 33103-22-9 恩维霉素

CAS Name: Tuberactinomycin N
Additional Names: (R)-1-[(3R,4R)-4-hydroxy-3,6-diaminohexanoic acid]-6-[L-2-(2-amino-1,4,5,6-tetrahydro-4-pyrimidinyl)glycine]viomycin
Percent Composition: C 43....
Literature References: Polypeptide antibiotic produced by a mutant of Streptomyces griseoverticillatus var. tuberacticus. Isoln and characterization: T. Ando et al., J. Antibiot. 24, 680 (1971); A. Nagata et al., in Advan. Antimicrob. Antineopl. Chemother. vol. 1/2, M. Hejzlar et al., Eds. (University Park Press, Baltimore, 1972) pp 1039-1041. Prepn: J. Abe et al., DE 2133181; eidem, US 3892732 (1972, 1975 both to Toyo Brewing Co., Ltd.). Structural studies: H. Yoshioka et al., Tetrahedron Lett. 1971, 2043; T. Wakamiya, T. Shiba, J. Antibiot. 28, 292 (1975). Pharmacology: H. Hamakawa et al., Oyo Yakuri 8, 817 (1974), C.A. 82, 51530y (1975). Metabolism: T. Shimizu et al., Jpn. J. Antibiot. 27, 279 (1974). Total synthesis: T. Shiba et al., J. Antibiot. 32, 1078 (1979).

Giractide CAS Registry Number: 24870-04-0 吉拉克肽

CAS Name: 1-Glycine-18-L-argininamide-a(1-18)-corticotropin
Percent Composition: C 54.14%, H 7.09%, N 21.47%, O 15.87%, S 1.45%
Literature References: Polypeptide corresp to the first 18 amino acid residues in corticotropin, in which the 1-serine is replaced by glycine. Prepn: H. Otsuka et al., Bull. Chem. Soc. Jpn. 43, 196 (1970); of the hexaacetate: eidem, JP 70 19061 (1970 to Shionogi), C.A. 73, 110138r (1970). Adrenocorticotropic potency in man: J. Clin. Endocrinol. Metab. 33, 355 (1971). Fluorometric study: T. Muraki et al., Experientia 32, 1605 (1976). Absorption: M. Hirata et al., Chem. Pharm. Bull. 26, 1061 (1978). Chromatographic studies: S. Terabe et al., J. Chromatogr. 172, 163 (1979); M. Schoeneshoefer, A. Fenner, ibid. 224, 472 (1981).

Relaxin CAS Registry Number: 9002-69-1

Trademarks: Cervilaxin; Releasin (formerly) (Warner-Chilcott)
Literature References: Polypeptide hormone secreted by the corpora lutea of many mammalian species during pregnancy; also produced in several non-mammalians, including the shark. Facilitates the birth process by causing a softening and lengthening of the pubic symphysis and cervix; also inhibits contraction of the uterus and may play a role in timing of parturition. First discovered in estrogen-primed guinea pigs: F. L. Hisaw, Proc. Soc. Exp. Biol. Med. 23, 661 (1926). Extraction from corpora lutea: Fevold et al., J. Am. Chem. Soc. 52, 3340 (1930); Albert et al., Endocrinology 40, 370 (1947); from pregnant rabbit serum: Abramowitz et al., Anat. Rec. 84, 456 (1942); cf. Hall, Newton, J. Physiol. 106, 18 (1947). Can be obtained commercially from pregnant sows' ovaries. Isoln procedure and purification by resin chromatography: Lehrman et al., J. Am. Pharm. Assoc. 44, 206 (1955); R. L. Kroc, G. E. Phillips, US 2852431; G. E. Phillips, US 2852432 (both 1958 to Warner-Lambert). Isoln from ovarian tissue using glacial acetic acid: Cohen, US 2930737 (1960 to Princeton Laboratories). Alternate method: Keck, US 3008878 (1961 to Thomae). Prepn from hog ovaries: Doczi, US 3096246 (1963 to Warner-Lambert). Porcine relaxin has a mol wt of approx 6000 and consists of two peptide chains, A and B, of 22 and 31 residues respectively, linked covalently by one intra- and two inter-chain disulfide bonds. Purification, characterization of porcine relaxin: O. D. Sherwood, E. O'Byrne, Arch. Biochem. Biophys. 160, 185 (1974). Structure of the A chain: C. Schwabe et al., Biochem. Biophys. Res. Commun. 70, 397 (1976); of the B chain: eidem, ibid. 75, 503 (1977). Relaxin is structurally homologous to insulin and related growth factors: R. A. Bradshaw, Rev. Biochem. 47, 191 (1978); S. Bedarkar et al., Nature 270, 449 (1977); N. Isaacs et al., ibid. 271, 278 (1978). Complete amino acid sequence of porcine relaxin: R. James et al., ibid. 267, 544 (1977); of rat: M. J. John et al., Endocrinology 108, 726 (1981). Isoln, characterization of relaxin from the sand tiger shark (Odontaspis taurus): J. W. Reinig et al., ibid. 109, 537 (1981); structure: L. K. Gowan et al., FEBS Lett. 129, 80 (1981). Demonstration of synthesis of rat relaxin as a preprorelaxin molecule with a connecting peptide of 105 amino acid residues, using molecular cloning: P. Hudson et al., Nature 291, 127 (1981). Structure of a genomic clone from which the amino acid sequence of biologically active human relaxin was predicted: eidem, ibid. 301, 628 (1983). Reviews: C. Schwabe et al., Recent Prog. Horm. Res. 34, 123-211 (1978); Ann. N.Y. Acad. Sci. 380, entitled "Relaxin: Structure, Function, and Evolution", B. G. Steinetz et al., Eds. (1982) pp 1-244.