Sanglier J J, Traber R, Buck R H, Hofmann H, Kobel H
Preclinical Research, Biotechnology, Sandoz Ltd., Basel, Switzerland.
J Antibiot (Tokyo). 1990 Jun;43(6):707-14. doi: 10.7164/antibiotics.43.707.
By mutagenic treatment of a strain of Tolypocladium inflatum, a cyclosporin non-producing mutant was obtained which accumulated the characteristic building unit of cyclosporins, (4R)-4-[(E)-2-butenyl]-4-methyl-L-threonine (abbreviation Bmt; systematic name: (2S,3R,4R,6E)-2-amino-3-hydroxy-4-methyl-6-octenoic acid) in free form. The isolation from a culture filtrate was performed by extraction, chromatographic separation and final crystallization from methanol - water. The structure and stereochemistry of this amino acid was determined by chemical transformation and correlation to dihydro-MeBmt, with known chirality [(2S,3R,4R)-3-hydroxy-4-methyl-2-methylamino-octanoic acid], obtained by hydrolysis of dihydrocyclosporin A.
通过对一株Inflatum顶头孢霉进行诱变处理，获得了一株不产生环孢菌素的突变体，该突变体以游离形式积累了环孢菌素的特征性结构单元，（4R）-4-[(E)-2-丁烯基]-4-甲基-L-苏氨酸（缩写为Bmt；系统名称：(2S,3R,4R,6E)-2-氨基-3-羟基-4-甲基-6-辛烯酸）。从培养滤液中的分离通过萃取、色谱分离以及最终从甲醇-水体系中结晶来进行。该氨基酸的结构和立体化学通过化学转化以及与二氢-MeBmt的关联来确定，二氢-MeBmt具有已知的手性[（2S,3R,4R）-3-羟基-4-甲基-2-甲基氨基辛酸]，它是通过二氢环孢菌素A水解得到的。
