945-24-4 (2,4-二氨基-6-羟甲基蝶啶,2,4-Pteridinediamine-6-methanol)

_92%

反应条件：

1.1 Reagents: Acetic acid Solvents: Water ; rt → 80 °C; 80 °C → 45 °C
1.2 Reagents: Ammonium hydroxide Solvents: Water ; pH 5.3 - 5.6

参考文献：

Preparation of methotrexate derivatives for treatment of autoimmune disease and cancer

, World Intellectual Property Organization, , ,

合成路线：1 步

1426393-09-0

_91%

反应条件：

1.1 Reagents: Oxygen Solvents: Methanol , Water ; 12 h, rt
1.2 Reagents: Sodium bicarbonate Solvents: Water ; pH 8

参考文献：

A process for preparing 6-(bromomethyl)-2,4-pteridinediamine

, China, , ,

合成路线：1 步

100462-86-0

_68%

反应条件：

1.1 Reagents: Acetic acid Solvents: Acetic acid ; 75 °C; 15 min, 75 - 80 °C; 80 °C → 45 °C
1.2 Reagents: Ammonium hydroxide Solvents: Water ; pH 6, 45 °C

参考文献：

Preparation of ornithine derivative ammonium salts for treating inflammatory diseases

, United States, , ,

合成路线：1 步

_66%

反应条件：

1.1 Reagents: Barium chloride Solvents: Water ; 10 min, 100 °C; 100 °C → rt
1.2 Reagents: Sodium acetate , L-Cysteine, hydrochloride, monohydrate , Oxygen Solvents: Water ; 24 h, rt

参考文献：

Antimicrobial diaminopteridine derivatives

, World Intellectual Property Organization, , ,

合成路线：1 步

_55%

反应条件：

1.1 Reagents: Barium chloride Solvents: Water ; 10 min, heated
1.2 Reagents: Sodium acetate Solvents: Water ; 24 h, rt

参考文献：

Process for preparation of tetrahydrofolic acid analogs

, China, , ,

合成路线：1 步

_55%

反应条件：

1.1 Reagents: Barium chloride Solvents: Water
1.2 Reagents: Sodium acetate Catalysts: L-(+)-Cysteine hydrochloride Solvents: Water

参考文献：

Process for making dihydrofolate reductase inhibitor γ-methylene-10-deazaaminopterin

, World Intellectual Property Organization, , ,

合成路线：1 步

522614-11-5

_54%

反应条件：

1.1 Reagents: Ammonia Solvents: Methanol , Water ; 24 h, rt

参考文献：

Pteridines. Part CXIII. Protection of pteridines

Yao, Qizineng; Pfleiderer, Wolfgang, Helvetica Chimica Acta, 2003, 86(1), 1-12

合成路线：1 步

反应条件：

1.1 Reagents: Sodium hydroxide Solvents: Water ; 3 h, < pH 7, rt

参考文献：

Antifolate linker-drugs and antibody-drug conjugates

, United States, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Sodium hydroxide Solvents: Water ; 5 min, rt; 30 min, rt

参考文献：

Antifolate-carrying nanoparticles and their use in medicine

, World Intellectual Property Organization, , ,

合成路线：1 步

参考文献：

Optimization of N-alkylation in the Synthesis of Methotrexate and Pteridine-based Derivatives Under Microwave-Irradiation

Quotadamo, Antonio; Linciano, Pasquale ; Costi, Maria Paola; Venturelli, Alberto, ChemistrySelect, 2019, 4(15), 4429-4433

合成路线：1 步

反应条件：

1.1 Reagents: Sodium hydroxide Solvents: Water ; pH 7, 21 °C

参考文献：

Synthesis and Evaluation of Hydrogen Peroxide Sensitive Prodrugs of Methotrexate and Aminopterin for the Treatment of Rheumatoid Arthritis

Peiro Cadahia, Jorge; Bondebjerg, Jon; Hansen, Christian A.; Previtali, Viola; Hansen, Anders E.; et al, Journal of Medicinal Chemistry, 2018, 61(8), 3503-3515

合成路线：1 步

反应条件：

1.1 Reagents: Sodium hydroxide Solvents: Water ; pH 7, 21 °C

参考文献：

Preparation of prodrugs of methotrexate and derivatives thereof activated by reactive oxygen species for use in the treatment of inflammatory diseases and cancer

, World Intellectual Property Organization, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Sodium bicarbonate

参考文献：

Preparation of vasculostatic agents and methods of use

, World Intellectual Property Organization, , ,

合成路线：1 步

参考文献：

Carboxypeptidase-mediated release of methotrexate from methotrexate α-peptides

Kuefner, Ulrike; Lohrmann, Ute; Montejano, Yolanda D.; Vitols, Karin S.; Huennekens, F. M., Biochemistry, 1989, 28(5), 2288-97

合成路线：1 步

参考文献：

2,4-Diamino-6-(hydroxymethyl)pteridine hydrobromide

, Romania, , ,

合成路线：1 步

反应条件：

1.1 Reagents: Oxygen

参考文献：

2,4-Diamino-6-hydroxymethylpteridine

, United States, , ,

合成路线：1 步

54798-28-6

113-00-8

反应条件：

1.1 Solvents: Methanol

参考文献：

Pteridines. XXXVIII. Synthesis of some 2,4-diamino-6-substituted methylpteridines. New route to pteroic acid

Taylor, Edward C.; Portnoy, Robert C.; Hochstetler, Douglass C.; Kobayashi, T., Journal of Organic Chemistry, 1975, 40(16), 2347-51

合成路线：1 步

参考文献：

Diaminopteridine derivatives

, United States, , ,

合成路线：1 步